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Background: Lornoxicam microspheres are promising for targeted, controlled, or extended drug release, and the incorporation of mucoadhesive properties can significantly enhance bioavailability and absorption. This study focuses on the development of bioadhesive microspheres utilizing the ionotropic gelation and emulsion crosslinking methods. Purpose: The primary aim of this research is to formulate bioadhesive microspheres of Lornoxicam using Sodium Alginate, Carbopol 934, and Chitosan as polymers, while simultaneously evaluating Lornoxicam’s interactions within Alginate-Carbopol 934 and Chitosan matrices through molecular dynamics simulations. Methods: Formulations T1 to T4 employed drug-to-polymer ratios of 1:1, 1:2, 1:3, and 1:4 for Sodium Alginate and Carbopol 934, while formulations T5 to T8 utilized the same ratios for Chitosan and glutaraldehyde as the crosslinking agent. Comprehensive assessments were conducted on particle size, drug entrapment efficiency, and dissolution rates. Molecular dynamics simulations were performed to analyze Lornoxicam’s interactions within the polymer matrices. Results: Formulation T7 emerged as the optimal formulation based on extensive evaluation tests. Molecular dynamics simulations revealed stable RMSD values for Lornoxicam across both matrices, with the Chitosan matrix displaying greater fluctuations. Notably, stronger hydrogen bond interactions were observed in the Chitosan matrix, which corresponded to a marginally higher binding energy than the Alginate-Carbopol 934 matrix. Conclusion: These findings indicate that Chitosan may significantly enhance the pharmaceutical potential of Lornoxicam as a drug delivery system, highlighting the need for further exploration of its therapeutic applications. [ABSTRACT FROM AUTHOR]

Introduction: Nonsteroidal anti-inflammatory drugs (NSAIDs), which inhibit prostaglandin synthesis, are used in many clinical areas. Although they are advantageous because of their analgesic, anti-inflammatory, and antipyretic properties, their effects on tissue healing are controversial. Dexketoprofen and lornoxicam are widely used, new-generation NSAIDs. However, their effects on fibroblasts, which are important for healing, are unknown. Herein, we aimed to investigate the effects of these two drugs on fibroblast viability, migration, and collagen expression. Methods: L929 mouse fibroblasts were cultured in vitro. Viability assays, wound-healing assays, and gene expression analyses were performed after 24 hours of treatment with lornoxicam and dexketoprofen at a 0-1-mM dosage. The viability test, wound-healing test, and gene expression analysis were performed using the MTT method, by calculating the closed area, and by qRT-PCR, respectively. Results: Lornoxicam and dexketoprofen at doses of 0-1 mM dose-dependently decreased viability, and changes in cell morphology were observed. Lornoxicam 1 µM and dexketoprofen 10 µM doses significantly reduced the migration rate of L929 cells compared with the control group (****p<0.0001). After 24 hours, COL1A1 expression in L929 cells was 0.027 and 0.015 when 1 and 10 µM of lornoxicam and dexketoprofen were applied. Discussion and Conclusion: Lornoxicam and dexketoprofen have negative effects on the viability, migration, and type 1 collagen synthesis of fibroblasts. Considering these negative effects on fibroblasts is crucial while using these drugs. [ABSTRACT FROM AUTHOR]

Purpose: This study aims to compare the efficacy of two non-steroidal anti-inflammatory agents (NSAIDs), namely lornoxicam and etodolac for controlling pain, edema and trismus after removal of lower impacted third molars. Materials and methods: A total of 20 patients comprised of both genders with bilateral impacted lower impacted third molars (in similar positions) was included in the present study. Patients were randomly assigned either to the lornoxicam group (8 mg of lornoxicam) or to the etodolac group (400 mg of etodolac). The drugs prescribed were handed out immediately after tooth extraction. Postoperative pain was assessed using visual analog scale (VAS). Edema was evaluated using reference lines on the face. Trismus was assessed using a caliper at maximum mouth opening (mm). Results: There was no significant difference in postoperative pain, trismus, and edema between lornoxicam and etodolac group (p > 0.05). Conclusions: Based on the results obtained in the present study, ıt has been verified that both lornoxicam and etodolac were adequately effective in the management of pain following third molar surgery. Lornoxicam and etodolac had similar impacts on pain, edema and trismus after impacted lower third molar surgical extractions. [ABSTRACT FROM AUTHOR]

Lornoxicam (LN) is a non-steroidal anti-inflammatory and analgesic drug of the oxicam class. As with other non-steroidal anti-inflammatory drugs, it has the same side effects of this group of drugs if they are taken orally such as gastrointestinal, renal and hepatic disorders. Besides, it binds extensively to plasma albumin (99%), has a relatively short plasma half-life (3 to 5 hrs) and undergoes first pass hepatic metabolism and gastrointestinal degradation upon oral administration. These drawbacks render LN a good candidate for local delivery via sustained release dosage forms. Therefore, LN mucoadhesive buccal films were prepared by the solvent casting method using different polymers, that is sodium carboxymethyl cellulose (Na CMC), hydroxypropylmethyl cellulose (HPMC), hydroxypropyl cellulose (HPC), gelatin, polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP) K-30. Differential scanning calorimetry (DSC) and infrared spectroscopy (IR) studies indicated the absence of any physical or chemical interaction of the drug with any of the used polymers. The prepared films were evaluated for their weight uniformity, thickness uniformity, swelling index, surface pH, folding endurance, in vitro drug release as well as mucoadhesion force. On the basis of the results obtained, it was deduced that the best formula of LN mucoadhesive buccal films was that containing a mixture of Na CMC, HPC and PVP; since it exhibited a high bioadhesive strength, a high percentage of drug release, a good folding endurance and a high swelling index. It can be finally concluded that mucoadhesive buccal films can be one of the alternatives available for administration of LN in order to minimize its side effects and avoid the disadvantages of parenteral and oral routes of administration. [ABSTRACT FROM AUTHOR]

Osteoarthritis is a bone and joint condition characterized pathologically by articular cartilage degenerative damage and can develop into a devastating and permanently disabling disorder. This investigation aimed to formulate the anti-inflammatory drug lornoxicam (LOR) into bile salt–enriched vesicles loaded in an in situ forming hydrogel as a potential local treatment of osteoarthritis. This was achieved by formulating LOR-loaded bilosomes that are also loaded with superparamagnetic iron oxide nanoparticles (SPIONs) for intra-muscular (IM) administration to improve joint targeting and localization by applying an external magnet to the joint. A 31.22 full factorial design was employed to develop the bilosomal dispersions and the optimized formula including SPION (LSB) was loaded into a thermosensitive hydrogel. Moreover, in vivo evaluation revealed that the IM administration of LSB combined with the application of an external magnet to the joint reversed carrageen-induced suppression in motor activity and osteoprotegerin by significantly reducing the elevations in mitogen-activated protein kinases, extracellular signal-regulated kinase, and receptor activator of nuclear factor kappa beta/osteoprotegerin expressions. In addition, the histopathological evaluation of knee joint tissues showed a remarkable improvement in the injured joint tissues. The results proved that the developed LSB could be a promising IM drug delivery system for osteoarthritis management. [ABSTRACT FROM AUTHOR]

Aim: This study focused on developing a topical gel incorporating lornoxicam-loaded poly(lactic-co-glycolic acid) and polyethylene glycol (PLGA-PEG) blend nanoparticles to mitigate gastrointestinal (GIT) side effects and enhance therapeutic efficacy. Materials & methods: Synthesized nanoparticles were subjected to in vitro characterization, ex vivo permeation studies, and acute oral toxicity analysis post-incorporation into the gel using a S/O/W double emulsion solvent. Results & conclusion: The nanoparticles displayed a smooth, spherical morphology (170–321 nm) with increased entrapment efficiency (96.2%). LOX exhibited a permeation rate of 70–94% from the nanoparticle-infused gel, demonstrating favorable biocompatibility at the cellular level. The formulated gel, enriched with nanoparticles, holds promising prospects for drug-delivery systems and promising improved therapeutic outcomes for LOX. GRAPHICAL ABSTRACT Article highlights Utilizing the S/O/W double emulsion solvent evaporation method, LOX-loaded PLGA-PEG nanoparticles were fabricated with a sustained release effect intended for topical use. The study evaluated the effects of dependent characteristics, such as encapsulation effectiveness, particle size, and percentage penetration of nanoparticles, on independent parameters, such as homogenization speed, and percentage of PEG and PLGA concentration. To evaluate the drug–polymer compatibility and interactions, a variety of methodologies, including FTIR analysis, ex vivo permeation, XRD acute oral toxicity analysis, surface morphology evaluation, percentage yield, and particle size assessment, were used to characterize the nanoparticles. A relationship between the PLGA concentration and these other responses was evident, as increasing the PLGA concentration resulted in larger nanoparticle sizes and increased encapsulation efficiency. In contrast, the effects of homogenization speed and PEG percentage on particle size and encapsulation efficiency decreased, indicating that higher homogenization speeds and percentages of PEG produced smaller nanoparticles with lower encapsulation effectiveness. The results of scanning electron microscopy showed smooth, spherical nanoparticles with appropriate boundaries. FTIR research confirmed that there was no drug–polymer interaction, confirming the compatibility of the components with the Carbapol 940 gel as well. Biocompatibility and safety profiling of the developed system were ensured by acute oral toxicity analysis. Skin penetration studies have shown that higher PLGA concentrations improve the topical sustained release impact of nanoparticles, whereas higher PEG percentages and faster homogenization lead to better skin penetration rates. As a result, gel-containing PLGA-PEG nanoparticles have become a viable option for topical medication delivery, providing advantages for improved penetration and sustained drug delivery. [ABSTRACT FROM AUTHOR]

Transdermal drug delivery is gaining importance as they are devoid of gastric issues and extended time. The synthetic polymers/excipients used in them are costlier and in the search of natural and abundant excipients. The goal of the existing work was to create matrix transdermal patches with lornoxicam (LXM) gel using lemon oil (LO) and Aloe vera leaves mucilage (AVLM) as penetration enhancers to boost LXM transport crossways the skin and test its in vivo analgesic effects. Nine formulas were produced for this purpose using Design Expert® 11 in line with CCD design. The response factors, on the other hand, were Q1d (Y1), Q2d (Y2) and Q3d, or LXM permeation at days 1, 2 and 3. As independent variables, the AVLM concentration (X1) and lemon oil (X2) were selected. The skin sensitivity response and analgesic activity of the optimized patch were tested on rats. The results exhibited that a matrix system with prolonged (zero-order) LXM release of 24.15% (@24h), 49.00% (@48h) and 69.45% (optimized optimised for the needed analgesic asset by using AVLM and LO as penetration enhancers. It was resolute that the formulation known as LTDP-8, which contains 3mL of AVLM and LO as permeability enhancers, is the best one. In light of its ability to administer LXM across the skin in a sustained manner while producing a tolerable analgesic effect. The study concludes that the artificial transdermal LXM delivery system is a suitable substitution for the oral route. [ABSTRACT FROM AUTHOR]

Targeted drug delivery (TDD) systems have several advantages, especially with drugs having toxic side effects such as lornoxicam (LX) which shows high hepatotoxicity and nephrotoxicity, especially with long-term use. This work represents an attempt to control magnetic microspheres encapsulating LX and magnetite nanoparticles (MNPs) for potential targeted drug delivery of LX. Superparamagnetic nanoparticles were fabricated via the co-precipitation method and together with LX were encapsulated into polycaprolactone (PCL) microspheres through an oilin-water (O/W) emulsion solvent evaporation method. The effects of changing the amount of drug, MNPs, and volume of the aqueous phase were investigated by preparing several microsphere formulations. Increasing the amount of encapsulated MNPs increased the magnetization of the microspheres without affecting the morphology. Doubling the volume of the aqueous phase resulted in a higher encapsulation efficiency and drug loading; 83.9% and 10.7%, respectively, while increasing the amount of drug had a negative effect on both drug loading and encapsulation efficiency. Drug release from the microspheres was successfully achieved and showed a biphasic nature. A system of four planar coils was then used to magnetically control the movement of a cluster of capsules in a glycerin medium, as a simulation for the targeting process. The microspheres were successfully controlled to move in a U-turn path with sharp corners demonstrating their potential for TDD applications. [ABSTRACT FROM AUTHOR]

Targeting the inflammation-related molecules with nonsteroidal anti-inflammatory drugs (NSAIDs) represents a promising approach for cancer prevention/therapy. We evaluated the in vitro anticancer effects of meloxicam, lornoxicam, ketoprofen, and dexketoprofen on the proliferation, migration, and apoptosis of human cervical, colorectal, and mammary carcinoma cells. The antiproliferative activity and cytotoxicity of tested NSAIDs on HeLa, HT-29, and MCF-7 cell lines were assessed by the MTT test. The apoptosis-inducing potential was analyzed by fluorescent staining with acridine orange/ethidium bromide and DAPI. Migration activity was assessed by a wound-healing scratch assay. The tested NSAIDs reduced the viability of the used tumor cell lines. The cytomorphological analysis revealed reduced cell density and mitotic activity and the presence of cells with morphological features of early and late apoptosis. Significant inhibition of the migration capacity was established as well. In conclusion, NSAIDs could be candidates for the development of new pharmacological strategies for the treatment and prevention of cancer. [ABSTRACT FROM AUTHOR]

The present study aimed to evaluate the impact of ultrafine nanoemulsions on the transdermal delivery of lornoxicam (LOR) for management of the inflammation. The transdermal administration of LORNE could increase the efficacy of LOR with a reduction in side effects. Merging the beneficial properties of ultrafine nanoemulsions and their components (penetration enhancers) can lead to good solubilization, a small droplet size, and more effective LOR carriers. Therefore, this study aims to develop and evaluate the potential use of ultrafine nanoemulsions of LOR (LORNE) to elucidate their skin targeting for the treatment of inflammation. Based on solubility and pseudo ternary phase diagram tests, ultrafine LORNE composed of Labrafil M 2125 CS, Cremophor RH40, and Transcutol HP to deliver LOR was developed and characterized for its physicochemical properties, emulsification, and in vitro release. The selected LORNE was incorporated into carbopol gel (LORNE-Gel) and examined for ex vivo skin permeation, retention, dermatokinetics, anti-inflammatory efficacy, and skin irritation. The selected LORNE12-Gel could improve skin permeation, retention, and dermatokinetic results significantly (p

Abstract Background Catheter-related bladder discomfort (CRBD is a painful complication of intraoperative urinary catheterization after anaesthesia. We conducted this study to compare the effect of tramadol and lornoxicam for the prevention of postoperative CRBD. Methods One-hundred twenty patients (aged 18–60 years, ASA physical status 1–2, undergoing elective uterine surgery requiring intraoperative urinary catheterization were randomly divided into three groups with 40 patients in each group. Group T received 1.5 mg/kg tramadol, group L received 8-mg lornoxicam, and group C received normal saline. The study drugs were administered intravenously at the end of the surgery. The incidence and severity of CRBD were reported at 0, 1, 2, and 6 h after arrival at the postanaesthesia care unit (PACU). Results The incidence of CRBD was significantly lower in groups T and L than in group C at 1, 2, and 6 h after surgery. The incidence of moderate to severe CRBD was also significantly lower in groups T and L than in group C at 0, 1, and 2 h after surgery. The severity of CRBD reported as mild, moderate, and severe was reduced in groups T and L compared with group C at most times after surgery. Group T had a higher incidence of nausea than group C, and there were no differences in dizziness, drowsiness, or vomit among the three groups. Conclusions Tramadol and lornoxicam administered intravenously at the end of the surgery were both effective in preventing the incidence and severity of CRBD after uterine surgery. However, tramadol increased the incidence of nausea compared with saline, but there was no difference between tramadol and lornoxicam. Trial registration ChiCTR2100052003. Registered on 12/10/2021.

In the current research, lornoxicam-loaded in situ gels were developed, and their potential usage in ocular inflammation was evaluated. Lornoxicam cyclodextrin complex prepared with hydroxypropyl methylcellulose and poloxamer P407 because of the low viscosity of in situ gels to provide easy application. However, washing and removing it from the ocular surface becomes difficult due to the gelation formation with heat. A three-level factorial experimental design was used to evaluate the effects of poloxamer 407 concentration, polymer type, and polymer concentration on viscosity, pH, gelation capacity, gelation time, and gelation temperature, which were considered the optimal indicators of lornoxicam-containing formulations. As a result of the three-level factorial experimental design, the optimized formulation contained 15 (%w/v) poloxamer 407 and 1 (%w/v) hydroxypropyl methylcellulose. The optimize formulation viscosity 25 °C = 504 ± 49cP, viscosity 35 °C = 11247 ± 214cP, pH = 6.80 ± 0.01, gelation temprature = 35 ± 0.2 °C, and gelation time= 34 ± 0.2 s was obtained. In the in vitro release studies, 68% of lornoxicam was released with a burst effect in the first three hours; then, the release continued for eight hours with controlled release. Release kinetics of the formulations were modeled mathematically, and it was found to be compatible with the Korsemeyer-Peppas and Weibull models. In cell culture studies, cell viability at 100 µg/mL was 83% and 96% for NL6 and NL6-CD, respectively. In Draize's in vivo test, no negative conditions occurred in rats. Therefore, the NL6-CD formulation has the potential to be a favorable option for treating ocular inflammation. [ABSTRACT FROM AUTHOR]

Lornoxicam was practically water insoluble and a nonsteroidal anti-inflammatory therapeutic agent thus associated with gastrointestinal tract (GIT) side effects. Lipid polymer hybrid nanocarriers (LPHNs)-based transdermal nanogel of lornoxicam was formulated to increase solubility of lornoxicam and sustained lornoxicam release that lead to eliminate GIT related side effect, prolong therapeutic activity and improve patient compliance .The lornoxicam LPHNs formulations (LH1-LH6) were prepared by microwaves based method. The conventional gel of lornoxicam (G) was prepared by solvent diffusion method. The LH1-LH6 was entered to characterization processes that were later used as a base to prepare lornoxicam hybrid nanogel formulations (LN1-LN6). The LN1-LN6 was tested for various evaluations. It was found that all the LH1-LH6 were show nanosize globules, low polydispersity index and acceptable surface charge, entrapment efficiency and drug loading. LH3 was the most optimized LPHNs due had lower particle size and higher lornoxicam release.The evaluation processes indicate stable organoleptic properties, high homogeneity, and acceptable values of pH. The comparability profile of the lornoxicam release from the lornoxicam nanogel formulations (LN1-LN6) and conventional lornoxicam gel (G) was in the following descending order: LN3 > LN2> LN1 > LN6 > LN5 > LN4 > G. The characterization and evaluation processes highly support promise transdermal delivery system to decrease pain and inflammation in musculoskeletal diseases.

Introduction: The most common complication following third molar surgery is pain. The purpose of the study is to determine the efficacy of lornoxicam as a preventive analgesic in patients undergoing surgical removal of impacted mandibular third molars. Materials and Methods: This study included 26 participants aged 18–28 years with bilateral symmetrical third molars. Group A, the control group, received lornoxicam 8 mg 1 h after surgery, whereas Group B, the study group, received lornoxicam 8 mg 1 h before surgery. All patients were evaluated for pain at the 1st, 2nd, 4th, 6th, 8th and 12th post-operative hours. The number of rescue analgesics taken within 24 h of the procedure, as well as the first occurrence of pain postoperatively, was recorded and analysed. Results: Using the Mann–Whitney U-test and Friedman's analysis, the resulting data were statistically analysed. When Group B was compared to Group A, there was a significant difference in pain reduction levels in the immediate post-operative hours. When compared to Group A, Group B had a lower need for rescue analgesics within the first 24 h postoperatively. Discussion: Following mandibular third molar surgery, pre-emptive use of lornoxicam is effective in reducing post-operative pain and reducing the need for rescue analgesic consumption. [ABSTRACT FROM AUTHOR]

Background: Catheter-related bladder discomfort (CRBD is a painful complication of intraoperative urinary catheterization after anaesthesia. We conducted this study to compare the effect of tramadol and lornoxicam for the prevention of postoperative CRBD. Methods: One-hundred twenty patients (aged 18–60 years, ASA physical status 1–2, undergoing elective uterine surgery requiring intraoperative urinary catheterization were randomly divided into three groups with 40 patients in each group. Group T received 1.5 mg/kg tramadol, group L received 8-mg lornoxicam, and group C received normal saline. The study drugs were administered intravenously at the end of the surgery. The incidence and severity of CRBD were reported at 0, 1, 2, and 6 h after arrival at the postanaesthesia care unit (PACU). Results: The incidence of CRBD was significantly lower in groups T and L than in group C at 1, 2, and 6 h after surgery. The incidence of moderate to severe CRBD was also significantly lower in groups T and L than in group C at 0, 1, and 2 h after surgery. The severity of CRBD reported as mild, moderate, and severe was reduced in groups T and L compared with group C at most times after surgery. Group T had a higher incidence of nausea than group C, and there were no differences in dizziness, drowsiness, or vomit among the three groups. Conclusions: Tramadol and lornoxicam administered intravenously at the end of the surgery were both effective in preventing the incidence and severity of CRBD after uterine surgery. However, tramadol increased the incidence of nausea compared with saline, but there was no difference between tramadol and lornoxicam. Trial registration: ChiCTR2100052003. Registered on 12/10/2021. [ABSTRACT FROM AUTHOR]

The present study aimed to evaluate the impact of ultrafine nanoemulsions on the transdermal delivery of lornoxicam (LOR) for management of the inflammation. The transdermal administration of LORNE could increase the efficacy of LOR with a reduction in side effects. Merging the beneficial properties of ultrafine nanoemulsions and their components (penetration enhancers) can lead to good solubilization, a small droplet size, and more effective LOR carriers. Therefore, this study aims to develop and evaluate the potential use of ultrafine nanoemulsions of LOR (LORNE) to elucidate their skin targeting for the treatment of inflammation. Based on solubility and pseudo ternary phase diagram tests, ultrafine LORNE composed of Labrafil M 2125 CS, Cremophor RH40, and Transcutol HP to deliver LOR was developed and characterized for its physicochemical properties, emulsification, and in vitro release. The selected LORNE was incorporated into carbopol gel (LORNE-Gel) and examined for ex vivo skin permeation, retention, dermatokinetics, anti-inflammatory efficacy, and skin irritation. The selected LORNE12-Gel could improve skin permeation, retention, and dermatokinetic results significantly (p < 0.05) with enhanced C Skin max and AUC 0-48h compared to LOR-Gel. Moreover, LORNE12-Gel showed a remarkable anti-inflammatory effect compared to LOR-Gel after topical application. No signs of skin irritation were observed following treatment, indicating the safety of LORNE12-Gel. Thus, this study demonstrated that LOR-loaded LORNE12-Gel could be promising as an efficient transdermal nanocarrier for an anti-inflammatory alternative. [ABSTRACT FROM AUTHOR]

Background and Aims: The current study aimed to develop an osmotic drug delivery system for Lornoxicam to prolong its release. Methods: Two different approaches were used for development of the osmotic drug delivery system; the first one was to formulate a controlled porosity osmotic tablet and the other was to design an elementary osmotic tablet. The controlled porosity osmotic tablets were coated with different concentrations of osmogents, a pore former, and varying coating thicknesses, and the effects were observed on the release. In the elementary osmotic pump, the tablets were drilled to make an orifice that creates pressure to release the drug by osmosis, and drug release was studied. Results: The formulations were evaluated for different parameters namely appearance, uniformity of weight, drug content, hardness, and drug release. Also, the effect of different osmotic agents responsible for developing the osmotic pressure such as sodium chloride and mannitol along with the different concentrations of pore-forming sorbitol were studied. A comparison was made between the controlled porosity osmotic tablet in which the membrane coating contains water-soluble poreforming polymers that leach when the membrane comes in contact with water thereby permitting water inside the wall and creating the osmotic pressure to release the drug, and the elementary osmotic tablet containing the osmotic agent sodium chloride coated with the rate-controlling semipermeable membrane, cellulose acetate, which contains an orifice of a critical size through which the drug is delivered. Conclusion: From the results, it was found that the developed formulation of the controlled porosity osmotic tablet was able to release Lornoxicam (CPOP) over 12 hours at zero-order kinetics and, the concentration of the osmotic agent, level of pore former, and thickness of the membrane coating are responsible for controlling the release of lornoxicam. The membrane coating was subjected to SEM analysis, which showed the formation of pores in the membrane. The developed controlled porosity osmotic pump tablet of lornoxicam was found to control the drug release for 12 hours. [ABSTRACT FROM AUTHOR]

The solubility data of Active Pharmaceutical Ingredients in organic solvents is an essential for pharmaceutical crystallization and drug formulation. In this work, two semi-empirical correlations- the Yaws model and λ-h modeland two thermodynamic models - Wilson Model and the Non-random two-liquid model-are used to estimate the solubility of lornoxicam in ethanol and water. The model parameters and correlations coefficients are calculated by optimizing the average relative deviation. The values of these parameters will be helpful to estimate the solubility of lornoxicam at different temperatures where the experimental solubility data is not available. The predicted solubility data of lornoxicam can be further utilized in the pharmaceutical crystallization and drug formulation. [ABSTRACT FROM AUTHOR]

The present study aims to design and optimize the lornoxicam dispersible tablet (LXDT) formulation using the Quality by design (QbD) approach. A randomized Box–Behnken experimental design was used to characterize the effect of the critical factors, such as filler (MCC/Mannitol) ratio, mixing time, and disintegrant concentration, and assessed for their impacts on the critical quality attributes (responses), including dispersibility time, friability, dissolution efficiency, and content uniformity, respectively. The drug-excipients interaction of the formulation was investigated using FTIR and DSC, respectively. The accelerated stability study at 40 °C/75% relative humidity was performed. FTIR revealed an absence of any significant chemical interaction in solid state. DSC thermogram suggested that LX endothermic peak was slightly decreased due to the dilution effect. LXDT formulations exhibited acceptable friability (0.2 to 0.9%). The dissolution efficiency of LXDT formulations ranged from 72.21 to 93.63%. The overall study showed that the optimum level of independent factors was found to be 3:1 MCC/Mannitol, 11 min mixing time, and 6.23% disintegrant concentration. Accelerated stability studies showed the compendial acceptable hardness, friability, and disintegration times. The application of QbD approach can help in the detailed understanding of the effect of CMAs and CPPs on the CQAs on LXDT final product. [ABSTRACT FROM AUTHOR]

Aim: This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches., Background: Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution., Objective: The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration., Method: Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties., Results: The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h., Conclusion: The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Introduction: This study aims to develop immediate release tablet formulations of lornoxicam (LRX) using hot melt extrusion (HME)-based fused deposition modeling (FDM) focusing on the adjustment of drug release by arranging infill densities and evaluating microcrystalline cellulose II (MCC II) as a disintegrating agent for HME-FDM purposes. LRX is a poorly soluble drug that exhibits pH-dependent solubility with a high thermal degradation temperature. These characteristics make it an ideal model drug for the HME-based FDM technique., Methods: Various filament formulations were extruded using an extruder, and suitable filaments were used to produce 3D-printed tablets. Filaments and tablets were characterized. Dissolution studies were performed on tablets with different infill densities. DSC, FTIR, XRD, and SEM analyses were conducted., Results: Although the solubility of LRX increases with pH, disintegrating agents such as MCC II had a more significant effect on the dissolution of LRX than sodium bicarbonate, which was used as the alkalinizing pore-forming agent. Dissolution studies revealed that the dissolution of LRX was enhanced by tablet erosion. Tablet erosion increased as the infill density decreased, and an immediate release profile was reached with tablets having 25% infill density. Despite the availability of conventional immediate release LRX tablets, this newly developed formulation offers the potential to be modulated for personalized therapy via the 3D printing technique., Conclusion: This study demonstrates the feasibility of HME-based FDM printing technology for producing immediate-release LRX tablets with consistent quality, highlighting the utilization of MCC II as a disintegrating agent that enhances LRX dissolution in this process.

Background: Mouth dissolving film (MDF) is a fast-dissolving drug delivery system that provides a practical means to administer drugs not just to special populations with swallowing difficulties but also to the general public. MDFs are novel dosage forms that dissolve and disintegrate quickly within the mouth. Aim: To assess the efficacy of lornoxicam mouth dissolving film as a potent analgesic and drug delivery system and compare it with the aceclofenac tablet in the management of post-extraction pain. Methodology: The study group comprised 60 subjects of either sex of age group 20–50 years who were divided into an experimental group (group A) and a control group (group B). Group A was administered lornoxicam MDF and group B was administered aceclofenac tablets. Pre-treatment and post-treatment pain assessments were recorded using a visual analog scale (VAS) and an oral pain scale (OPS). Results: In a comparison of the mean value of pre-treatment VAS and VAS after 24 h, the percentage of pain reduction in group A was 86.66%, and in group B was 75%. When comparing the mean value of pre-treatment OPS and OPS after 24 h, the percentage of pain reduction in group A was 93.33% and in group B was 75%. These results were statistically significant, with a P value of 0.00 in both groups. Conclusion: Lornoxicam as an MDF showed promising results in managing post-extraction pain. The potential delivery of lornoxicam through the MDF was safe, with better patient compliance, and no reported cases of adverse effects.

INTRODUCTION: Nonsteroidal anti-inflammatory drugs have become a popular part of multimodal analgesic regimens particularly in ambulatory surgery. This study was designed to search the efficacy of preoperative administration of lornoxicam or paracetamol in patients who underwent open inguinal hernia repair. MATERIALS AND METHODS: American Society of Anesthesiologists Classification (ASA) I–III male patients with unilateral primary inguinal hernia scheduled for elective prosthetic repair under general anesthesia were randomly assigned to three groups. Group I patients were infused 100-ml normal saline 30 min before anesthesia (placebo), whereas Group II and Group III patients were given 8 mg lornoxicam or 1,000 mg paracetamol intravenously in 100-ml normal saline. Postoperative pain was treated with patient controlled intravenous morphine. Postoperative pain scores were evaluated with visual analog scale (VAS) in the recovery room and at 1st, 6th, 12th, and 24th hours postoperatively in all groups. Total amount of analgesics. Liker scale and SF-36 form was also used at 4th week follow-up in order assess quality of life. RESULTS: Totally 88 patients were completed the study (G1 = 28, G2 = 30, and G3 = 30). Preemptive use of both lornoxicam and paracetamol resulted in significantly lower recovery room VAS scores in comparison with placebo group (3.93, 3.73, and 5.25). Both lornoxicam and paracetamol groups (G2 and G3) displayed better results at 12th h than placebo group (P = 0.04). VAS scores at 24th hour were similar in three groups. Total morphine consumptions were also similar between the groups at all times. Total postoperative 1-week oral analgesic use was significantly less in G2 (lornoxicam), and G3 (paracetamol) in comparison with G1 (placebo). Quality of life indicators in Likert Scale and SF-36 form were also not different. CONCLUSION: Preemptive use of both lornoxicam and paracetamol may be effective in early postoperative pain control in patients undergo elective open inguinal hernia repair. However, there seems to be no difference between the efficacies of the two agents.

Lornoxicam physiologically based pharmacokinetic (PBPK) models were developed and validated on the basis of clinical pharmacokinetic results obtained by considering CYP2C9 genetic polymorphisms in healthy adult populations. PBPK models were extended to predict lornoxicam pharmacokinetics for patients with cirrhosis by quantitatively examining the pathophysiological information associated with cirrhosis. The predicted plasma exposure to lornoxicam was approximately 1.12–2.83 times higher in the CYP2C9*1/*3 and *1/*13 groups than in the CYP2C9*1/*1 group of healthy adult populations and patients with cirrhosis. The predicted plasma exposure to lornoxicam was approximately 1.28–3.61 times higher in patients with cirrhosis than in healthy adult populations. If the relationship between lornoxicam exposure in plasma and drug efficacy was proportional, then the proposed adjusted doses of lornoxicam for each group varied from 1.25 mg to 8 mg. As the severity of cirrhosis increased, or when the CYP2C9 genotype was *1 heterozygous, the dose adjustment range of lornoxicam increased. Therefore, the effect of pathophysiological factors (cirrhosis severity) on the pharmacokinetics of lornoxicam might be more important than that of CYP2C9 genetic factors. These results could be useful for broadening the scope of clinical application of lornoxicam by enabling dose selection based on CYP2C9 genotypes and liver cirrhosis degree. [ABSTRACT FROM AUTHOR]

Background: In the medical and pharmaceutical fields, man has successfully used natural-origin things for millennia. Polymers obtained from plant sources have flashed much consideration in current eras owing to their various pharmaceutical properties, such as gelling agents in gels. Also incorporated in cosmo products, fabrics, dyes, and paper manufacture as binders, diluents, disintegrating agents, thickeners in oral fluids, protective colloids in suspensions, and bases in a suppository. Objectives: Natural polymers are chosen over semisynthetic and synthetic excipients due to their lack of toxicity, low cost, availability, soothing action, and nonirritant nature, as well as their ability to undergo a variety of chemical modifications. However, they have some drawbacks, including microbial contamination, lot to lot variation, reduced viscosity throughout storage, inappropriate mechanical properties, low storage, and an uninhibited rate of hydration. Current research work aims to chemically modify xanthan gum and study its impact on the formulation of topical gels. Materials and Methods: Chemical modification of xanthan gum is conceded by using a thiol-esterification reaction with thioglycolic acid (TGA) in the presence of hydrochloric acid. Microwave irradiated thiolated xanthan gum was also willing by further irradiation of thiolated xanthan gum by microwave using 750 W frequency. Topical drug delivery of lornoxicam release applications of thiolated and microwave irradiated xanthan gum are comparatively evaluated with pure xanthan gum polymer by formulating gel incorporated lornoxicam as a drug. Results: The physical properties of gel-like physical evaluation and viscosity results are within official limits. Formation of gel with idyllic properties. Determination of drug content, spreadability, and extrudability of modified xanthan gum was high compared with native xanthan gum. In vitro drug release study showed that prepared gel sustains the drug release for 24 h. Conclusion: Thiolation and irradiated xanthan gum sustain the release of lornoxicam over a prolonged period and might be a promising lornoxicam carrier in topical drug delivery to enhance antinociceptive and anti-inflammatory efficiency. [ABSTRACT FROM AUTHOR]

Xiaohua Zhang,1,&ast; Xinguo Liu,2,&ast; Qiongxiang Ye,2 Xunbao Wang,2 Jinjun Chen,2 Zhiyong Wang,2 Pengfei Zhao,2 Baozhou Tao,2 Guoping Xu,2 Wanfeng Xu,2 Kan Wu,2 Yao Xiao,3 Li Yang,1 Junqiang Tian,1 Juan Wang,1 Zhilong Dong,1 Zhiping Wang1 1Institute of Urology, Lanzhou University Second Hospital; Key Laboratory of Gansu Province for Urological Diseases; Gansu Nephro-Urological Clinical Center, Lanzhou, Gansu Province, People’s Republic of China; 2Department of Urology, Susong County People’s Hospital, Susong, Anhui Province, People’s Republic of China; 3Department of Pediatrics, Lanzhou University Second Hospital, Lanzhou, Gansu Province, People’s Republic of China&ast;These authors contributed equally to this workCorrespondence: Zhiping Wang Email wangzplzu@163.comObjective: To compare the analgesic efficacy and safety of acupuncture and lornoxicam in acute renal colic (ARC).Design, Setting, Participant: A randomized, double-blind, parallel-controlled, single-centered trial was conducted at Susong County People’s Hospital from October 2019 to November 2020. Eighty-four patients with ARC were randomly divided into lornoxicam group (Group L) and acupuncture group (Group A). Group A was treated with acupuncture at Sanyinjiao (SP6), Yinlingquan (SP9) and normal saline, and Group L was treated with sham acupuncture at SP6, SP9 and lornoxicam.Main Outcome Measures: Visual analogue scale (VAS) scores and adverse reactions such as nausea and dizziness were recorded within 5, 10, 15, 20 and 40 minutes after treatment. The main outcome of this study was the short-term effective (STE) rate, the secondary outcome was the onset time, and the safety index was incidence of adverse reactions.Results: A total of 80 patients completed this study, including 41 patients (21 males and 20 females) in Group L and 39 patients (21 males and 18 females) in Group A. Group A exhibited lower scores versus group L after treatment (P < 0.05). The overall STE of group L was 61.00% (25/41), significantly lower than group A [84.62% (33/39)] (P < 0.001). There was no difference in the incidence of adverse reactions between group A [2.6% (1/39)] and group L [7.3% (3/41)] (P = 0.616). The ordered logistic regression analysis showed patients receiving acupuncture therapy are more likely to be cured [OR = 2.887, 95% CI: (1.190, 7.000), P = 0.019].Conclusion: Acupuncture at SP6, SP9 and intramuscular injection of lornoxicam can effectively and safely relieve ARC, but the former has faster and better analgesic effect. Moreover, the incidence of adverse reactions was similar between the two treatments. This acupuncture therapy is recommended as a complementary therapy for ARC.Keywords: acupuncture, lornoxicam, renal colic, analgesia

Mahmoud H Teaima,1 Khaled M Abdel-Haleem,2 Rewan Osama,2 Mohamed A El-Nabarawi,1 Osama S Elnahas2 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, EgyptCorrespondence: Mahmoud H TeaimaDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, EgyptTel +201005840264Email mahmoud.teaima@pharma.cu.edu.egSignificance: Statins are an important class of drugs that help to control hyperlipidemia, and one of these statins recently used is pitavastatin calcium (PITA). Nevertheless, the most reported adverse effect of statins is myopathy. Therefore, combining statins with non-steroidal anti-inflammatory drugs (NSAIDs) as Lornoxicam (LORNO) can help in the management of statin-induced myopathy.Purpose: This study aimed to formulate and evaluate different oral disintegrating tablets (ODTs) containing PITA using different co-processed excipients. The best PITA-ODT was selected and reformulated with the addition of LORNO, forming a single ODT comprising both drugs. The pharmacokinetic parameters of PITA and LORNO in a single ODT were compared to those of the marketed products (Lipidalon® and Lornoxicam®).Methods: Eight PITA-ODTs were prepared via direct compression. The prepared PITA-ODTs were evaluated for their weight variation, thickness, breaking force, friability, drug content, and wetting time (WT). In-vitro disintegration time (DT) and dissolution were also evaluated and taken as parameters for selection of the best formula based on the criteria of scoring the fastest DT and highest Q10 min. LORNO was added to the selected PITA-ODT, forming a single ODT (M1) comprising both drugs, which was subjected to an in-vivo pharmacokinetic study using rats as an animal model and liquid chromatography-mass spectrometry (LC-MS/MS) for analysis of both drugs in rat plasma.Results: Results showed that all PITA-ODTs had acceptable physical properties in accordance with pharmacospecial standards. PITA-ODT prepared with Pharmaburst® (F2) had significantly (p< 0.05) the fastest DT (6.66± 1.52 s) and highest Q10 min (79.07± 2.02%) and was chosen as the best formula. The in-vivo pharmacokinetic study of M1 formula showed higher percent relative bioavailability (%RB) of 286.7% and 169.73% for PITA and LORNO, respectively, compared with the marketed products.Conclusion: The single ODT comprising PITA and LORNO was promising for instant co-delivery of both drugs with higher %RB when compared with the marketed products.Keywords: oral disintegrating tablets, co-processed excipients, pitavastatin calcium, Lornoxicam, in-vivo pharmacokinetic study, liquid chromatography-mass spectrometry

Abstract Background Tonsillectomy is one of the most common procedures in otorhinolaryngology practice where analgesics are required for pain-relief especially in children. To compare the efficacy of using peritonsillar infiltration of lidocaine Hcl versus intravenous preincisional lornoxicam in reducing post tonsillectomy pain. Results Prospective, randomized, double-blinded, placebo-controlled study. Ninety-nine patients from age 12 to 18 years old, prepared for tonsillectomy. Patients were randomly subdivided into three groups as 33 patient in each group to receive either lidocaine (group 1), lornoxicam (group 2), or saline as a placebo (group 3). Anesthesia was induced using intravenous fentanyl and propofol, while endotracheal intubation was facilitated with rocuronium and maintenance by halothan. Intraoperative bleeding, pain scores, interval until first order for analgesic. The postoperative complications including bleeding, hypoxia, nausea, and vomiting also were observed. Pain scores at rest were significantly lower in group 2 than groups 1 and 3 at all observation times. Similarly, pain scores were lower in group 2 during the first 5 postoperative hours. The mean time for rescue analgesic was 276 min in group 2, 91 min in group 1, and about 60 min in group 3. No significant differences were noted for intraoperative bleeding. Conclusion The use of lornoxicam 16 mg at preoperative phase gave good control of immediate post tonsillectomy pain. Level of evidence 3b

The study aims to (a) enhance the solubility of a poorly soluble drug by optimization of nanocrystal formulation using the top-down approach and (b) modify the release profile of this drug, which exhibits a short elimination half-life, by the integration of a fast-release phase containing the optimized nanocrystals and a sustained-release phase in a compression-coated tablet. Nanocrystals of the model drug (lornoxicam; LNX) was prepared by simultaneous application of jet-milling and ball-milling techniques. Investigation of the precipitation inhibition capacity, thermal property, and interaction of different polymers with the drug revealed polyvinyl pyrrolidone K30 (PVP) as the most effective stabilizer for nanocrystals. The immediate-release layer containing the optimized nanocrystals (size of 279.5 ± 11.25 nm and polydispersity index of 0.204 ± 0.01) was then compressed on a zero-order sustained-release matrix core using different derivatives of hydroxypropyl methylcellulose (HPMC). Application of the Design of Experiment approach (DoE) was applied to optimize the formulation of tablet. Analysis of drug concentration in dog plasma by liquid chromatography-tandem mass spectrometry demonstrated an improvement in the release behavior of LNX from the optimal compression-coated tablet integrating a HPMC-based sustained release matrix core and a PVP-stabilized lornoxicam nanocrystals coating layer compared to the reference product. [ABSTRACT FROM AUTHOR]

Nanoemulsions are promising drug delivery systems for the administration of poorly soluble drugs like lornoxicam (LRX) by oral or parenteral routes. Such formulations work perfectly for transdermal delivery of lornoxicam-type drugs. It has also been established that formulating such a delivery system is highly dependent on the presence, type, and concentration of excipients taking part in the formulation. The inherent characteristics of nanoemulsion (NE), i.e., smaller globule size and excipient nature, facilitate the drug's passage through skin. The current study was aimed at the development of an NE-based formulation of LRX to improve the drug solubility in vitro as well as to enhance drug skin permeation to promote therapeutic outcome in appropriate time. Spontaneous self-emulsification technique was utilized to develop optimized LRX-encapsulated NE-based formulations. ATR-FTIR spectra of the pure drug and various formulations did not show any interaction between the drug and various formulation excipients showing compatibility. Globule size for stable formulations ranged between 63–168 nm. These formulations were characterized for viscosity, surface tension, pH, drug encapsulation efficiency, in vitro drug release, and drug skin permeation studies. Chitosan-decorated optimized NE formulation of LRX showed about 58.82% cumulative drug release, showing an anomalous non-Fickian diffusion mechanism of drug release. Drug encapsulation efficiency, in vitro drug release, and skin permeation studies exhibited promising results. An appreciable drug entrapment efficiency was exhibited by optimized NE formulations LRX-6, 71.91 ± 3.17% and C-LRX, 65.25 ± 4.89%. Permeability parameters like enhancement ratio (Er), permeability constant (Kp), and steady state flux (Jss) showed higher values and exhibited good results based on formulation type. The selected promising formulation type "LRX-6" showed significantly different results as compared to other formulations (LRX-4, 5, and 7). The skin permeation property of the LRX-6 formulation was compared to similar chitosan-based formulations and was found to have better skin permeation results than chitosan-based formulations. This study clearly exhibited that an LRX-containing NE-based formulation can be formulated to form a stable drug delivery system. Such formulations are promising in terms of physicochemical characteristics, improved solubility, and high skin permeation potential. [ABSTRACT FROM AUTHOR]

An economical and eco-friendly hydrothermal method for the preparation of nitrogen-doped carbon quantum dots (N-CQDs) was studied with rambutan peel and lysine. The morphology, structure, and optical properties of N-CQDs were characterized by transmission electron microscopy, Fourier transform infrared spectrometry, X-ray powder diffractometer, X-ray photoelectron spectrometry, and UV spectrophotometry. The synthesized N-CQDs have excellent characteristics such as strong fluorescence, good dispersion, high stability, and excellent water solubility. The absolute fluorescence quantum yield is 1.02%, the average particle size is 1.63 nm, and the maximum excitation wavelength is 340 nm. The maximum emission wavelengths are 430 nm and 800 nm. As a quencher, lornoxicam (LNX) was used to quench the fluorescence of N-CQDs with the mechanism of inner filter effect. The fluorescence ratio of N-CQDs (F430/F800) shows a good linear relationship to the concentration of LNX. The linear range and the detection limit of LNX are 0.01‒100 and 0.003 μmol/L, respectively. An effective ratiometric fluorescence probe for the detection of LNX was constructed. The method has the advantages of low detection limit, high sensitivity, wide linear range, and can be applied to the determination of LNX in real samples. Moreover, according to the excitation-dependent fluorescence behavior, dual-wavelength emission, and biocompatibility of N-CQDs, it has been applied to cell imaging. [ABSTRACT FROM AUTHOR]

Background: In the medical and pharmaceutical fields, man has made successful use of natural origin things for millennia. Natural medications and excipients have piqued the interest of the entire globe today. Obtained from plant polymers have flashed a lot of attention in current decades because of their various pharmacological applications, such as gelling agents in gels as well as in, cosmo products, tablets, oral fluids, suspensions, and bases in a suppository. Objectives: Polymers are biocompatible, inexpensive, readily existing, and they are chosen over semisynthetic and artificial excipients. However, they have some drawbacks, including microbial contamination, lot to lot variation, reduced viscosity throughout storage, inappropriate mechanical properties, low strew and uninhibited rate of hydration. Materials and Methods: The thiolesterification technique, which uses thioglycolic acid (TGA) in the presence of a catalytic quantity of hydrochloric acid, was used to modify xanthan gum chemically. Microwave irradiated thiolated xanthan gum was also made by irradiating thiolated xanthan gum with a 750W frequency after it had been microwave irradiated. Modified and crude xanthan gum was used to make the sustained release tablet of Lornoxicam. Pre-compression and post-compression tests were performed on compressed tablets. Results: FT-IR, DSC, and X-ray diffraction investigations all show that grafting was successful. Additional peaks were identified in thiolated Xanthan gum and microwave irradiated gum, which were not present in pure Xanthan gum, according to FT-IR research. The presence of the SH stretch of the thiol group may be seen in the bands closer to 2568.00 cm-1 and 2584.70 cm-1. Modified xanthan gum had a high swelling index. When compared to tablets made from crude xanthan gum, an in-vitro release study utilizing a pH 6.8 phosphate buffer indicated a sustain release of Lornoxicam from modified xanthan gum. Conclusion: Chemically modified xanthan gum sustains the drug over a prolonged period and could be a promising carrier in oral delivery to enhance anti-nociceptive and anti-inflammatory efficiency. [ABSTRACT FROM AUTHOR]

New screen-printed sensor with a boron-doped diamond working electrode (SP/BDDE) was fabricated using a large-area linear antenna microwave chemical deposition vapor system (LA-MWCVD) with a novel precursor composition. It combines the advantages of disposable printed sensors, such as tailored design, low cost, and easy mass production, with excellent electrochemical properties of BDDE, including a wide available potential window, low background currents, chemical resistance, and resistance to passivation. The newly prepared SP/BDDEs were characterized by scanning electron microscopy (SEM) and Raman spectroscopy. Their electrochemical properties were investigated by cyclic voltammetry and electrochemical impedance spectroscopy using inner sphere ([Fe(CN)6]4−/3−) and outer sphere ([Ru(NH3)6]2+/3+) redox probes. Moreover, the applicability of these new sensors was verified by analysis of the anti-inflammatory drug lornoxicam in model and pharmaceutical samples. Using optimized differential pulse voltammetry in Britton–Robinson buffer of pH 3, detection limits for lornoxicam were 9 × 10−8 mol L−1. The oxidation mechanism of lornoxicam was investigated using bulk electrolysis and online electrochemical cell with mass spectrometry; nine distinct reaction steps and corresponding products and intermediates were identified. [ABSTRACT FROM AUTHOR]

The present study was conducted to fabricate and compare pH-sensitive polymeric networks of Artemisia vulgaris- Methacrylic acid using free radical polymerization conventional method and microwave-assisted method. Potassium persulphate and N’ N’- Methylene bisacrylamide were employed as an initiator-crosslinker system. Swelling studies were performed at pH 1.2, 4.5, 6.8 and 7.4. Concentrations of polymer and monomer along with radiation dose were optimized as a function of swelling. Porosity and gel fraction were calculated for all samples. FTIR study confirmed the formation of cross-linked networks. Results of SEM indicated that the microwave irradiated polymeric network had a more porous structure. DSC and XRD study indicated the entrapment of drug inside the polymeric networks in amorphous form. In comparison to the conventional method, the polymeric network prepared by the microwave-assisted method exhibited high swelling ratios, porosity, thermal stability and drug release. These results signify microwave radiations as an effective alternative to the conventional heating method. [ABSTRACT FROM AUTHOR]

Sadek Ahmed, Mohamed Aly Kassem,† Sinar Sayed Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt†Mohamed Kassem, passed away on August 21, 2020Correspondence: Sinar SayedFaculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo 11562, EgyptTel +2 0 1010421543Email sinar.fouad@pharma.cu.edu.egPurpose: The goal of this research was to enhance the transdermal delivery of lornoxicam (LX), using nanovesicular carriers composed of the bile salt sodium deoxycholate (SDC), soybean phosphatidyl choline (SPC) and a permeation enhancer limonene.Methods: Thin-film hydration was the technique employed for the fabrication using a Box–Behnken design with three central points. The investigated factors were SPC molar concentration, SDC amount in mg and limonene percentage (%). The studied responses were percent entrapment efficiency (%EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and in vitro drug release (after 2, 10 h). In order to obtain the optimum formula, numerical optimization by Design-Expert® software was used. Electing the optimized bilosomal formula was based on boosting %EE, ZP (as absolute value) and in vitro drug release, taking in consideration diminishing PS and PDI. Further assessment of the selected formula was achieved by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), stability testing, ex vivo skin permeation and deposition. The in vivo pharmacodynamics activities of the optimized formula were examined on male rats and mice and compared to that of the oral market product.Results: The optimized bilosomal formula demonstrated to be nonirritant, with noticeably enhanced anti-inflammatory and antinociceptive activities. Superior in vivo permeation was proved by confocal laser scanning microscopy (CLSM).Conclusion: The outcomes demonstrated that bilosomes could improve transdermal delivery of lornoxicam.Keywords: lornoxicam, permeation enhancer, factorial design, confocal laser scanning microscopy, antinociceptive

During life, neck pain occurs in 20-70% of people, its prevalence in the total population is 4.9%, and the annual morbidity varies from 30 to 70%. Neck pain significantly reduces the quality of life and can lead to disability. It was found that the economic burden of neck pain is high and is associated with the amount of money spent on treatment, with «lost profits» due to employee illness, compensation for examinations and sick leave. Over the past decade, there has been an increase in the prevalence of neck pain, which increases the importance of improving the diagnostics, prevention and treatment of neck pain. Depending on the duration, neck pain is classified as acute, subacute and chronic. Neck pain may be non-specific (skeletal-muscular), secondary (specific, symptomatic) or associated with discogenic radiculopathy or cervical myelopathy. Nonspecific neck pain is the most common. Effective treatment of nonspecific neck pain includes therapeutic gymnastics, manual therapy, recommendations on lifestyle, activity and ergonomics in the organization of the workplace. Identification and correction of risk factors of neck pain occurrence, persistence and chronization are of great importance in the prevention and treatment of patients. Neck pain pharmacotherapy includes drugs from the group of non-steroidal anti-inflammatory drugs (NSAIDs): lor-noxicam, which has shown its effectiveness and good tolerance in the treatment of neck pain, cervicocranialgia, postoperative and skeletal-muscular pain. It is recommended to prescribe a short course of NSAIDs therapy in minimal therapeutic doses. In the chronic course of neck pain, antidepressants may be prescribed, especially when combined with depression.

Abstract Background The goal of the proposed study was to validate a rapid, simple, an accurate, robust, and sensitive bioanalytical method for quantifying Meloxicam and Lornoxicam (as internal standard) in rabbit plasma. Result Limit of detection and limit of quantification for Meloxicam were found to be 0.0081 and 0.1035 μg mL−1, respectively. The bioanalysis was continued according to standard guidelines and successfully used for bioavailability studies of meloxicam after single dose administration of pure drug and the formulation in rabbit plasma. Finally, obtained results proved its simplicity and an efficiency to be applied for the therapeutic drug monitoring and bioequivalence studies. Conclusion Therefore, the set RP-HPLC bioanalysis is simple, convenient, and acceptable to analyze meloxicam in bulk and pharmaceutical formulations in rabbit plasma. Graphical abstract

Osteoarthritis is a chronic joint disease characterized by chronic inflammation, progressive destruction of articular cartilage, and subchondral bone sclerosis. When compared to individual treatment, the combined administration of genes and small-molecule drugs for osteoarthritis may not only provide superior inflammation control and pain relief, but may also repair cartilage damage. Here, cationic liposomes (CL) were used to deliver small hydrophobic drugs and microRNA into chondrocytes to treat osteoarthritis. Lornoxicam cationic liposomes (Lnxc-CL) were prepared by film dispersion, and loaded with microRNA-140 (miR-140) by electrostatic interaction to obtain cationic liposomes co-loaded with lornoxicam and miR-140 (Lnxc-CL/miR-140). The prepared Lnxc-CL/miR-140 had a particle size of 286.6 ± 7.3 nm, polydispersity index (PDI) of 0.261 ± 0.029 and zeta potential of 26.5 ± 0.5 mV and protected miR-140 from RNase degradation for 24 h. Lnxc-CL/miR-140 was evaluated for its ability to regulate gene expression in chondrocytes in vitro and to provide in vivo therapeutic effects for knee osteoarthritis in rats. The results of in vitro uptake experiments and polymerase chain reaction (PCR) analysis showed that Lnxc-CL/miR-140 efficiently delivered miR-140 into chondrocytes and up-regulated the expression of miR-140 and COL2A1 mRNA. Pharmacodynamics studies demonstrated that Lnxc-CL/miR-140 effectively treated osteoarthritis by eliminating joint inflammation and repairing damaged cartilage cells, with superior therapeutic effects compared to Lnxc or miR-140 alone. Overall, the findings of this study support the co-delivery of Lnxc and miR-140 with cationic liposomes as a potential new therapeutic strategy for the treatment of osteoarthritis. [ABSTRACT FROM AUTHOR]

Background/Aim: Preventing sensitization by an analgesic administered before a painful stimulus is the basis for preemptive analgesia. Preemptive use of pain medication prior to the application of painful stimuli results in better-controlled pain. This study aimed to compare the effects of preoperatively administered low-dose ketamine and lornoxicam on postoperative analgesia, their side effects and patient satisfaction in orthopedic operations on the lower extremities. Methods: Seventy-eight patients aged 18-70 years who were admitted for lower extremity surgery under general anesthesia were enrolled in this prospective, randomized, and double-blind study. The patients were randomly allocated to one of the three following groups: Four milliliters of physiological saline were administered to the patients in Group P, 0.15 mg kg-1 ketamine was given to the patients in Group K and 8 mg lornoxicam was administered to those in Group L, all in 4 ml of volume, intravenously, 15 minutes before anesthesia induction. Postoperative pain was evaluated at rest and during movement at 0th, 2nd, 4th, 6th, 8th, 12th, 20th and 24th postoperative hours with the Visual Analogue Scale (VAS) and the Verbal Pain Scale (VPS). Total fentanyl consumption, additional meperidine usage, side effects and patient satisfaction were recorded at these times. Results: The mean area under the VAS and VPS at rest and movement-time curves were lower in Group K compared to the other groups. Group P and Group L were comparable in terms of the area under the VAS at rest and movement-time curves, but the mean area under the VPS at rest and movement-time curves were higher in Group P compared to Group L. Total fentanyl consumption was lower in Group K than the other two groups (P=0.001). Conclusion: Low-dose ketamine administered preoperatively to patients for lower extremity surgery decreased postoperative pain scores more than lornoxicam or placebo. [ABSTRACT FROM AUTHOR]

[Display omitted] This study introduces two innovative nanocarrier systems to improve oral drug delivery. Desosomes and desimicelles combine Deep eutectic solvent (DES) with vesicular or micellar nanosystems, respectively. These novel nanosystems integrate the DES solubilization potency for administering drugs with low aqueous solubility and the vesicular and micellar systems to bypass physiological barriers and improve poor drug bioavailability. Lornoxicam (LRX) is a BCS class II anti-inflammatory with limited aqueous solubility and rapid clearance. Desosomes and desimicelles were prepared and successfully optimized. The optimization depended on particle size, zetapotential, entrapment efficiency, and solubility. The optimized desosomes (LRX-DES-V) and desimicelles (LRX-DES-M) were pictured by transmission electron microscope. Differential scanning calorimetry (DSC) and FTIR analysis indicated the successful inclusion of LRX inside each system. Invitro LRX release profiles revealed controlled release of LRX-DES-V and LRX-DES-M, with more sustained release by the later one. In-vivo study, inflammation was induced using a carrageenan rat model, and the anti-inflammatory effect of LRX-pure, marketed product, traditional niosomes, LRX-DES-V & LRX-DES-M were determined using inhibition %, serum inflammatory cytokines, and histopathology. After 4 h of induction, LRX-DES-M (68.05%) showed a significant inhibition compared to LRX-DES-V (63.57%). LRX-DES-M also showed a better reduction in COX2, PGE2, and TNF-α (1.25-fold, 1.24-fold, and 1.36-fold inhibition), respectively, compared to LRX-DES-V. We can conclude that LRX-DES-V and LRX-DES-M showed better effects than all other groups and that LRX-DES-M might be more effective than LRX-DES-V. [ABSTRACT FROM AUTHOR]

Gastrointestinal tract (GIT) side effects due to the local action of lornoxicam considered the most common problem that associated with using of this analgesic drug. Masking of the enolic alcohol OH group of lornoxicam to overcoming this problem was the aim, however, applying Williamson ether synthesis led to amide hydrolysis. Therefore, the objective of this study was shifted to study the hydrolytic kinetics and the influence of different bases as a function of time and temperature in the reaction media. The effects of all bases used in the study on the hydrolysis process of lornoxicam have been studied; NaOH was found to be the strongest followed by Na2CO3 and K2CO3. All three temperatures (25°C, 50°C and 80°C) have approximately similar effect except reflux condition that accelerates the hydrolysis process compare with the others. The hydrolysis process is proportional with time. Williamson ether synthetic procedure that followed to synthesize lornoxicam prodrugs was failed despite attempting different conditions. Using bases were induced the hydrolysis process of lornoxicam. The hydrolysis rate accelerated under reflux more than other conditions. In addition, reaction time gives more hydrolysis process.

Shanshan Gao, Baocheng Tian, Jingtian Han, Jing Zhang, Yanan Shi, Qingzhi Lv, Keke LiSchool of Pharmacy, Binzhou Medical University, Yantai, People’s Republic of chinaBackground: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The surface modification of NLCs with cell-penetrating peptides (CPPs) can enhance the skin permeation of drugs.Purpose: The objective of the current study was to evaluate the ability of the cell-penetrating peptide (CPP) polyarginine to translocate NLCs loaded with lornoxicam (LN) into the skin layers and to evaluate its anti-inflammatory effect.Methods: The NLCs were prepared using an emulsion evaporation and low temperature solidification technique using glyceryl monostearates, triglycerides, DOGS-NTA-Ni lipids and surfactants, and then six histidine-tagged polyarginine containing 11 arginine (R11) peptides was modified on the surface of NLCs.Results: The developed NLCs formulated with LN and R11 (LN-NLC-R11) were incorporated into 2% HPMC gels. NLCs were prepared with a particle size of (121.81±3.61)–(145.72±4.78) nm, and the zeta potential decreased from (−30.30±2.07) to (−14.66±0.74) mV after the modification of R11 peptides. The encapsulation efficiency and drug loading were (74.61±1.13) % and (7.92±0.33) %, respectively, regardless of the surface modification. Cellular uptake assays using HaCaT cells suggested that the NLC modified with R11 (0.02%, w/w) significantly enhanced the cell internalization of nanoparticles relative to unmodified NLCs (P

A selective and sensitive reverse phase High Performance Liquid Chromatographic method has been developed and validated for the estimation of lornoxicam in bulk, pharmaceutical dosage forms and in dissolution samples. The analysis was performed isocratically on an Inertsil column (250* 4.6 mm, 5 pm) using a mass spectrometric compatible mobile phase of 10 mM ammonium acetate: acetonitrile (50:50 V/V) at a flow rate of 1 mL/min. The detection wavelength was 290 nm. The retention time was found to be 4.573 min for lornoxicam. The linearity of the method has been satisfied with Beer Lambert's law in the concentration range of 5-25 µg/mL with a correlation coefficient of 0.9988. The mean recoveries assessed for lornoxicam were in the range of 100.39-101.86 %, indicating good accuracy of the method. The limit of detection and limit of quantification were found to be 0.03 and 0.11 µg/mL, respectively. The developed method has been statistically validated in accordance with ICH guidelines and found to be mass spectrometric compatible, simple, precise, and accurate with the prescribed values. Thus, the proposed method was successfully applied for the estimation of lornoxicam in routine quality control analysis of bulk, formulations and in dissolution samples. [ABSTRACT FROM AUTHOR]