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The present study was aimed to develop chitosan-coated enamel adhesive device of CAP-P 407 (Cellulose acetate phthalate-Poloxamer 407), loaded with MNC (Minocycline) for sustained release and site-specific drug delivery system for the carious lesion. The average tensile strength and in-vitro drug release of uncoated dental film were found to be 15.97 kg/mm2 and 98.11% in 24 h, respectively. The average in-vitro mucoadhesion time and tooth adhesion strength of the finished product was found to be 249 minutes and 268 g, respectively. In-vitro antimicrobial study showed the drug concentration is well above MIC even after 8 hours of drug release. [ABSTRACT FROM AUTHOR]

Obesity is a complex, multifactorial, lifestyle-related disorder which affects nearly one-third of the global population. In more than one way, obesity classifies as a potential indicator or contributing factor of various clinical conditions, subsequently leading to poor health outcomes and compromised quality of life (QoL). The high prevalence and reporting rate of obesity is irrespective of geographical difference, ethnicity and gender, however, they most often serve as predisposing risk factors for obesity. Additionally, environmental changes, availability & affordability of low nutrition, yet palatable food, hormonal disbalance and variation at the genetic level, prominently exacerbates the condition of obesity and its related effects. Clinically, obesity, may either lead to other pathophysiological conditions as well, such as liver dysfunction, polycystic ovarian syndrome, hypertension, coronary artery diseases and psychological impairment or vice-versa. Henceforth, to cope with the challenges of obesity and related conditions, a healthy lifestyle, personal care & social well-being is of prime importance. Additionally, a customized strategy to address the economic expenditure and newer therapeutic perspectives should be implemented to control the widespread damage of human population by this condition. The present review focuses on providing a brief knowledge about nutritional, biochemical, genetic and psychological aspects of obesity and its epidemiology. [ABSTRACT FROM AUTHOR]

The bio-analytical method was developed and validated for simultaneous detection and quantification of paclitaxel (PAC) and erlotinib (ERL) in plasma samples. The sample preparation process was accomplished by liquid-liquid extraction technique. The dried and reconstituted samples were subjected to chromatography on Discovery -C18 (50 × 4.6 × 5µm) column and a mobile phase, composed of a mixture of 0.1% formic acid in water: acetonitrile (70:30, v/v), in isocratic mode at a flow rate of 0.6 mL/min. Liquid chromatography coupled to tandem mass spectrometry detection in positive ion mode was selected to provide optimal selectivity and sensitivity. The mass transitions of erlotinib, erlotinib13C6, Paclitaxel and docetaxel were m/z 394.5→278.4, m/z 400.4→284.5, m/z 876.6→308.4 and m/z 830.0→304.0 respectively. The linearity in the calibration curves was obtained in the concentration range of 3.6 − 1006.7 ng/ml (r ≥ 0.99) for erlotinib and 5.3 − 1500.0 ng/mL for paclitaxel with an LLOQ (lower limit of quantification) of 3.6 and 5.3 ng/ml respectively. The run time was achieved in 2.5 min only, for all the analytes. [ABSTRACT FROM AUTHOR]

Mass consumerization of three-dimensional (3D) printing innovation has revolutionised admittance of 3D-printing in an expansive scope of ventures. When utilised predominantly for industrial manufacturing, 3D-printing strategies have rapidly attained acquaintance in different parts of health care industry. 3D-printing is a moderately new technology that has discovered promising applications in the medication conveyance and clinical areas. This review intends to explore different parts of 3D- printing innovation concerning pharmaceutical and clinical applications. Review on pharmaceutical products like tablets, caplets, films, polypills, microdots, biodegradable patches, medical devices (uterine and subcutaneous), patient specific implants, cardiovascular stents, etc. and prosthetics/anatomical structures, surgical models, organs and tissues created utilising 3D-printing is being presented. In addition, the regulatory understanding and current IP and clinical trial status pertaining to 3D fabricated products/medical applications have also been funnelled, garnering information from different web portals of regulatory agencies and databases. It is additionally certain that for such new innovations, there would be difficulties and questions before these are acknowledged as protected and viable. The circumstance demands purposeful and wary endeavours to acquire regulations which would at last prompt the accomplishment of this progressive innovation, thus various regulatory challenges faced have been conscientiously discussed. [ABSTRACT FROM AUTHOR]

The major drawback of the eye drops is rapid elimination of drug from the precorneal region, thus ensuing poor bioavailability as well as therapeutic efficacy. To conquer these limitations, a pH triggered in situ gel was developed for sustained delivery of levofloxacin. Two polymers namely hydroxypropyl methylcellulose (HPMC) and sodium alginate along with the boric acid buffer were used to formulate the in situ gel. Based on the various physicochemical evaluation parameters like pH, clarity and gelling capacity placebo formulations were selected and further characterized for viscosity, in vitro release, ex vivo corneal permeation, and histopathological studies. The optimized in situ gel (F28) showed sustained release of 93 ± 4.23% for 24 h and cumulative drug permeation of 71.81 ± 4.7% for 72 h. Additionally, ocular irritation study and histopathology of the formulation treated cornea confirm the non-irritancy of the optimized formulation. Based on all the above performed studies, it can be concluded that the in situ gel would present a fruitful alternative for the ocular infections. [ABSTRACT FROM AUTHOR]

Despite the ongoing extensive research, cancer therapeutics still remains an area with unmet needs which is hampered by shortfall in the development of newer medicines. The present study discusses a nano-based combinational approach for treating solid tumor. Dual-loaded nanoparticles encapsulating gemcitabine HCl (GM) and simvastatin (SV) were fabricated by double emulsion solvent evaporation method and optimized. Optimized nanoparticles showed a particle size of 258 ± 2.4 nm, polydispersity index of 0.32 ± 0.052, and zeta potential of −12.5 mV. The size and the morphology of the particles wee further confirmed by transmission electron microscopy (TEM) and scanning electron microscopy, respectively of the particles. The entrapment efficiency of GM and SV in the nanoparticles was 38.5 ± 4.5% and 72.2 ± 5.6%, respectively. The in vitro release profile was studied for 60 h and showed Higuchi release pattern. The cell toxicity was done using MTT assay and lower IC50 was obtained with the nanoparticles as compared to the pure drug. The bioavailability of GM and SV in PLGA nanoparticles was enhanced by 1.4-fold and 1.3-fold respectively, compared to drug solution. The results revealed that co-delivery of GM and SV could be used for its oral delivery for the effective treatment of pancreatic cancer. [ABSTRACT FROM AUTHOR]

The present study was conducted for the optimization of transethosomes formulation for dermal fisetin delivery. The optimization of the formulation was carried out using "Box-Behnken design". The independent variables were Lipoid S 100, ethanol and sodium cholate. The prepared formulations were characterized for vesicle size, entrapment efficiency and in vitro skin penetration study. The vesicles-skin interaction, confocal laser scanning microscopy and dermatokinetic studies were performed with optimized formulation. Results of the present study demonstrated that the optimized formulation presented vesicle size of 74.21 ± 2.65 nm, zeta potential of −11.0 mV, entrapment efficiency of 68.31 ± 1.48% and flux of 4.13 ± 0.17 µg/cm2/h. The TEM image of optimized formulation exhibited sealed and spherical shape vesicles. Results of thermoanalytical techniques demonstrated that the prepared transethosomes vesicles formulation had fluidized the rigid membrane of rat's skin for smoother penetration of fisetin transethosomes. The confocal study results presented well distribution and penetration of Rhodamine B loaded transethosomes vesicles formulation up to deeper layers of the rat's skin as compared to the Rhodamine B-hydro alcoholic solution. Present study data revealed that the developed transethosomes vesicles formulation was found to be a potentially useful drug carrier for fisetin dermal delivery. [ABSTRACT FROM AUTHOR]

The study reports a rapid and short analytical technique for separation, characterization, and quantitation along with comparative pharmacological effect of curcuminoids in cerebral ischemia. Flash chromatography, using silica and diol columns along with gradient mobile phase, was utilized to separate three curcuminoids, i.e., curcumin (Cur), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC) for the first time. The separated peaks were monitored at 200–360 nm, whereas the purity of compounds (96.2–97.6%) was determined through qualitative analysis such as infrared and 1H and 13C-nuclear magnetic resonance spectroscopy, mass spectrometry (MS), and differential scanning calorimetry. Furthermore, chitosan nanoparticles (CS-NPs) for curcuminoids were prepared and characterized through zeta sizer, zeta potential, scanning electron microscopy, and transmission electron microscopy. The developed ultra performance of liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry/mass spectrometry (UPLC-ESI-Q-TOF-MS/MS) method showed simplified automation and shorter run time for Combi flash over conventional separation techniques. The CS-NPs for all the three curcuminoids and combined-curcuminoids (CCr) (combined and administered together for a synergistic effect), following intranasal administration in middle cerebral artery–occluded rats were evaluated for grip strength, locomotor activity, and histopathological examination where the anti-ischemic activity was observed, in terms of potency, for all three CS-NPs and CCr as CCr>Cur>DMC>>BDMC. Cur-CS-NPs exhibited more potency among Cur, DMC, and BDMC, whereas CCr was the more potent anti-ischemic drug compared to Cur, DMC, and BDMC. For Cur the characteristic activity is proposed because of the presence of methoxy group on the phenyl ring whereas for CCr it is synergistic effect of curcuminoids. [ABSTRACT FROM AUTHOR]

Efficient drug delivery at vaginal cavity is often a challenge owing to its peculiar physiological variations including vast differences in pH. Keeping in view this attribute of the target site, the current work was aimed at developing formulation strategies which could overcome this and successfully deliver molecules like itraconazole through SLNs. Optimized SLNs with the given composition was selected for further development into mucoadhesive and thermosensitive gel. Stearic acid and Compritol 888 (1:1, w/w ratio) as lipid, a mixture of 3% Poloxomer 188 and 0.5% sodium taurocholate as surfactant and organic to aqueous ratio of 10:50 was taken. Carbopol 934 and Pluronic F 127 were taken for the development of gel. Optimized gel exhibited a desired gelling temperature (35 °C); viscosity (0.920 PaS) and appreciablein vitrodrug release (62.2% in 20 h). MTT assay did not show any cytotoxic effect of the gel. When evaluatedin vivo,it did not exhibit any irritation potential despite appreciable bioadhesion. A remarkable decrease in CFUs was also observed in comparison with control and marketed formulation when evaluated in rat infection model. Thus, the proposed study defines the challenges for developing a suitable formulation system overcoming the delivery barriers of the vaginal site. [ABSTRACT FROM PUBLISHER]

Topotecan (TPT) is indicated against a variety of solid tumors, but has restricted clinical use owing to associated pharmaceutical caveats. This study is focused at formulating a successful TPT PLGA nanosystem which ameliorates the rapid conversion of active lactone form of drug to its inactive carboxylate form and consequently improvises its efficacy. TPT PLGA nanoparticles were formulated by a double emulsion-solvent evaporation technique with sequential optimization to obtain desired particle size, PDI, zeta potential, and entrapment efficiency. Stability of TPT was ensured by maintaining an acidic pH in the drug-containing phase and the system was evaluated forin vitro–in vivoperformance including cytotoxic potency. The optimized nanosystem had a particle size of 187.33 ± 7.50 nm, a PDI of 0.179 ± 0.05, and an entrapment efficiency of 56 ± 1.2%. Low pH in the interior of nanoparticles stabilized the drug to remain in its active lactone form and revealed a biphasic release pattern till 15 d. Additionally, anin vitrocytotoxicity testing as well asin vivoantitumor efficacy demonstrated a significant potential of higher proliferation inhibition as compared with neat drug (TPT). Thus, the investigation summarized an innovative simple tool for developing stable TPT NPs for effective delivery for treating solid tumors. [ABSTRACT FROM PUBLISHER]

Stroke is a one of the leading causes of disease and deaths worldwide, which causes irreversible deterioration of the central nervous system. Curcuminoids are reported to have a potential role in the amelioration of cerebral ischemia but they exhibit low serum and tissue levels due to low solubility and poor absorption. Curcumin (CUR), demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC)-loaded PNIPAM nanoparticles (NPs) were prepared by free radical polymerization and characterized for particles size, entrapment efficiency, zeta potential,in vitrorelease andex vivopermeation study. Optimized CUR, DMC and BDMC-loaded NPs had the mean size of 92.46 ± 2.8, 91.23 ± 4.2 and 94.28 ± 1.91 nm; zeta potential of −16.2 ± 1.42, −15.6 ± 1.33 and −16.6 ± 1.21 mV; loading capacity of 39.31 ± 3.7, 38.91 ± 3.6 and 40.61 ± 3.6% and entrapment efficiency of 84.63 ± 4.2, 84.71 ± 3.99 and 85.73 ± 4.31%, respectively. Ultra-performance liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectroscopy based bioanalytical method was developed and validated for pharmacokinetics, biodistribution, brain-targeting efficiency and brain drug-targeting potential studies post-intranasal (i.n.) administration which showed enhanced bioavailability of curcuminoids in brain as compared to intravenous administration. Improved neurobehavioural activity (locomotor and grip strength) and reduced cytokines levels (TNF-α and IL-1β) was observed in middle cerebral artery occlusion induced cerebral ischemic rats after i.n. administration of curcuminoids NPs. Finally, the toxicity study was performed which revealed safe nature of developed NPs. [ABSTRACT FROM AUTHOR]

The current investigation aims to present a novel solid lipid-based nanoparticulate system of resveratrol (RV) for the effective treatment of liver cirrhosis. A simplified solvent injection method was employed and the Box–Behnken experimental design was applied for optimization to get a window particle size of 150–200 nm having maximum entrapment efficiency as well as % release. Optimized resveratrol solid lipid nanoparticles (RV-SLNs) (SR-1) of appropriate characteristics (particle size = 191.1 ± 10.44 nm; zeta potential= −13.56 ± 4.14 mV; entrapment efficiency = 75.23 ± 3.85%; maximum % release = 80.53 ± 3.99%) were produced. Differential scanning calorimetry and X-ray diffraction studies were carried out which collectively proved the reduced crystallinity and stability enhancing the effect of the SLNs. Improved drug stability was further established by the appreciable shelf-life of the formulation from International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH)-recommended accelerated stability studies.In vivostudies revealed nearly five-fold increase in the bioavailability of SR-1 (AUC0→∞=3411 ± 170.34 µg/ml/h) as compared to RV suspension (AUC0→∞=653.5 ± 30.10 µg/ml/h). Pharmacodynamic data exhibited a significant decrease in the serum biomarker enzymes (serum glutamic oxalo-acetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT) and alkaline phosphatase) after oral administration of RV-SLNs as compared to control and marketed (SILYBON®) formulations against paracetamol-induced liver cirrhosis. The effect of the treatment was confirmed by the histopathology of the liver microtome sections. Finally, reverse transcriptase-polymerase chain reaction studies were conducted on isolated liver mRNA from SR-1 treated animals and significant down-regulation of tissue inhibitor of metalloproteinases-1 and nuclear factor-kB was witnessed. [ABSTRACT FROM PUBLISHER]

A receptor level interaction of etoposide with P-glycoprotein (P-gp) and subsequent intestinal efflux has an adverse effect on its oral absorption. The present work is aimed to enhance the bioavailability of etoposide by co-administering it with quercetin (a P-gp inhibitor) in dual-loaded polymeric nanoparticle formulation. Poly-lactic-co-glycolic acid (PLGA) nanoparticles were optimized for various parameters like o/w phase volume ratio, poly-vinyl alcohol concentration, PLGA concentration and sonication time. The cytotoxicity studies (MTT assay) revealed a 9- and 11-fold decrease in the IC 50 values for etoposide-loaded nanoparticles (ENP) and etoposide + quercetin dual-loaded nanoparticles (EQNP) when compared to that of free etoposide, respectively, and the results were further supported by florescent-activated cell sorter studies. The confocal imaging of the intestinal sections treated with ENP and EQNP containing fluorescent probe (rhodamine) showed the superiority of the EQNP to permeate deeper. Furthermore, pharmacokinetic studies on rats revealed that EQNP exhibited a 2.4-fold increase in bioavailability of etoposide than ENP with no quercetin. The developed loaded nanoparticles have the high potential to enhance the bioavailability of the etoposide and sensitize the resistant cells. [ABSTRACT FROM AUTHOR]

A sensitive, selective, precise, and stability-indicating, high-performance, thin-layer chromatographic (HPTLC) method for analysis of sertraline, both as a bulk drug and in house formulation, was developed and validated. The method employed thin-layer chromatographic (TLC) aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of Toulene/Ethyl acetate/Ammonia (1:5:0.1, v/v) as a mobile phase. The densitometric analysis were carried out at 273 nm using Camag TLC scanner which generated compact spots for SRT (Rf = 0.70 ± 0.02). The linear regression data for the calibration plots showed good linear relationship with r2 = 0.998 in the concentration range of 25–2000 ng spot−1. Sertraline was subjected to acid and alkali hydrolysis, oxidation, photodegradation, and dry heat treatment. Also, the degraded products were well separated from the pure drug. The method was validated for precision, accuracy, ruggedness, and recovery. As the method could effectively separate the drug from its degradation products, it can be employed as a stability indicating one. Moreover, the proposed HPTLC method was utilized to investigate the kinetics of acid and base degradation process. [ABSTRACT FROM AUTHOR]

The oral delivery of hydrophobic drug presents a major challenge because of the low aqueous solubility of such compounds. Self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. The efficiency of oral absorption of said drug from such type of formulation depends on many formulation-related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-emulsifying systems. With the growing interest in this field, there is an increasing need for guidelines in excipient selection to obtain effective delivery system with improved bioavailability. The aim of this review is to present the recent approaches in selecting the most appropriate lipid system(s); methods for its characterization and role of various excipients for improved delivery of dosage form. [ABSTRACT FROM AUTHOR]

CD44 or hyaluronan receptor is a transmembrane receptor associated with aggressive tumour growth, proliferation, and metastasis. In normal physiology, this receptor has a crucial role in cell adhesion, inflammation, and repair processes. However, many tumour cells over-express this receptor and abuse it to become progressive and perpetual units. The article comments from common functioning of the CD44 receptor, to its diabolic multi-dimensional effects in promotion of malignant cells. It also illuminates the relations of CD44 endorsed processes with other biomolecular events in cancer progression. In an end, the review focuses comprehensively at ongoing researches to exploit the CD44 over-expression as a probable target in treatment, management, and diagnosis of malignancy. [ABSTRACT FROM AUTHOR]

A stability-indicating high-performance thin-layer chromatographic (HPTLC) method was developed and validated for quantifying Itraconazole (Itz) in bulk drug, marketed formulation, and an in-house formulation comprised of lipidic-nano particle incorporated into vaginal gel. Aluminum plates precoated with silica gel 60 F-254 were used for TLC with Toulene:Ethyl acetate:Ammonia (1:5:0.1 v/v) as a mobile phase. The densitometric analysis was carried out at 266 nm using a Camag TLC scanner that generated compact spots for Itz (R f =0.77 ± 0.02). The regression analysis data for the calibration curve exhibited good linearity (r2 = 0.996 ± 0.0058). The LOD and LOQ values were found to be 14.29 ng spot−1 and 43.31 ng spot−1, respectively, while their recovery (99.65–100.23%) and precision (1.47%) were found to be satisfactory. Itraconazole was also subjected to forced stress conditions such as hydrolysis (acid and alkali), oxidation, dry and wet heat degradation, and photo degradation. The degradants were further characterized by NMR and Mass spectroscopy and compared with neat drug. Statistical analysis revealed that the developed method has potential for routine analysis of Itz in various formulations. It is well suited for quality control and study of pharmaceutical parameters such as release profile, loading, and entrapment in lipidic nanoparticle formulation. [ABSTRACT FROM AUTHOR]

A simple, sensitive, precise, and accurate stability-indicating high performance thin-layer chromatographic method for analysis of irinotecan both as bulk drug and in marketed injectables has been developed and validated as per ICH guidelines. Chromatographic separation was achieved on LiChrospher aluminum plates precoated with silica gel 60F254 as stationary phase. The solvent system consisted of acetone-ethyl acetate-acetic acid 8.5:1.5:0.1 (v/v/v) and this system was found to give compact spots for irinotecan at RF value of 0.31 ± 0.02. Densitometric analysis was performed in the absorbance at 366 nm. The linear regression analysis for the calibration plots showed good linear relationship with r2 = 0.9973 ± 0.0013 in the concentration range of 50-500 ng/spot. The method was validated for precision, accuracy, recovery, and specificity. The % recovery (94.63-101.40%) and precision (≤4.30) were found to be satisfactory. Irinotecan was subjected to acid and alkali hydrolysis, oxidation, thermal, and ultraviolet radiation treatments. All the peaks of degradation products were well resolved from the standard drug with significantly different retention factor (RF) values. Developed method effectively separated out the drug from its degradation products and hence can be used as stability-indicating method as well as in routine analysis of irinotecan. [ABSTRACT FROM AUTHOR]

Context: Humic acid (HA) is omnipresent in natural organic matter that is a macromolecular, negatively charged polyelectrolyte that contains a hydrophobic core. It is also present in a significant amount in Shilajit (used frequently in traditional medicines), which is used in this study as a source of extraction. HA is evaluated for the oral drug delivery of carbamazepine (CBZ). Objective: HA is used in this study to increase the dissolution, intestinal permeation, and pharmacodynamic response of CBZ (bio pharmaceutics classification system (BCS) II) by the technique of complexation and other related mechanism reported with humic substances. Methods: Different complexation techniques were explored in this study for the entrapment of CBZ, which was authenticated by molecular modeling and conformational analysis. These were further characterized using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and X-ray diffraction (XRD). Solubility analysis and dissolution release profile were carried out to access the in vitro parameters. For ex vivo studies, rat gut intestinal permeability was done. And finally pharmacodynamic evaluation (maximal electroshock method) was carried out for optimized complexes. Results: Molecular modeling approach and instrumental analysis (DSC, XRD, and FT-IR) confirmed the entrapment of CBZ inside the complexing agent. Increased solubility (∼1742%), sustained release (∼78%), better permeability (∼3.5 times), and enhanced pharmacodynamic responses conferred the best to 1:2 freeze dried (FD) and then 1:2 kneading (KD) complexes compared with pure CBZ. Conclusion: Now it could be concluded that HA may be tried as a complexing agent for antiepileptic drug and other classes of low water-soluble drug. [ABSTRACT FROM AUTHOR]

The aim of the present study was to formulate non-ionic surfactant vesicles of frusemide to enhance its skin permeation and to develop a transdermal therapeutic system using provesicular approach. The effect of various formulation variables on the transdermal flux, amount of drug deposited in skin, and plasma level of drug were studied. The skin permeation studies were conducted on rat skin and human skin for quantification of permeation parameters. With PGS3 formulation [Span 40:soyalecithin:cholesterol (4.5:4.5:1)], the plasma level in the rats had reached to a level of 0.42 ± 0.13 µg/mL at the sampling interval of 4 hr and remained within the therapeutic concentration range (1.66-0.3 µg/mL) for the next 12 hr. Results showed that proniosomal formulation was able to sustain the drug level in the blood and offer a promising means for non-invasive delivery of frusemide. [ABSTRACT FROM AUTHOR]

Amiloride hydrochloride, a generally used diuretic recently has been found effective in the treatment of epilepsy. The side effects of the drug, such as hyperkalemia, hypertension, and hyperaldosteronism were controlled by reducing the dose and targeting the drug to the brain. The objective of this study was to determine the factors influencing encapsulation of amiloride hydrochloride in liposomes and to demonstrate the anti-epileptic potential of liposomal drug. A series of liposomal formulations of amiloride hydrochloride were prepared by varying the compositions of the formulations. The optimized formulation consisted of 10 mg/mL of amiloride hydrochloride, L-phosphatidyl choline, lecithin, cholesterol, and butylated hydroxy toulene. The percentage entrapment efficiency in the optimized formulation was 44%. The drug to lipids ratio and L-phosphatidyl choline: lecithin: cholesterol: butylated hydroxy toulene ratios were 2.0:3.0 and 5:5:5:2, respectively. The formulation showed an in vitro release of 98.17% in 8 hours, and the best fit kinetic model was Peppas model. Treatment with amiloride hydrochloride liposomes resulted in a significant increase in seizure threshold as compared to free drug in increasing current electroshock seizures in mice, which indicated an increase in CNS uptake of drug in liposome formulation. [ABSTRACT FROM AUTHOR]

The present study describes stress degradation studies on a biomarker, trigonelline following the International Conference on Harmonization (ICH) guidelines under different stress conditions and establishment of a stability-indicating HPTLC assay method. Analysis of trigonelline was performed on TLC aluminium plates precoated with silica gel 60F-254 and mobile phase consisting of n-propanol-methanol-water (4:1:4 v/v/v). Spectrodensitometric scanning was carried out in absorbance mode at 269 nm for trigonelline (Rf=0.46±0.02). Trigonelline was subjected to acid and alkali hydrolysis, oxidation, dry heat, wet heat treatment, and photodegradation. Statistical analysis proves that the developed HPTLC method is reproducible and selective. As the method could effectively separate the drug from its degradation products, it can be employed as a stability-indicating one. Moreover, the method was utilized to investigate the kinetics of the acidic and alkaline degradation processes at different temperatures and to study degradation in constant ionic strength buffer solutions within the pH range 1–11. [ABSTRACT FROM AUTHOR]

Abstract The current work aims to develop a bigel-containing clobetasol propionate-loaded PLGA microparticles and further assess its in vitro, ex vivo, and in vivo behavior for psoriasis management. PLGA microparticles (2%w/w) containing clobetasol propionate were developed by solvent evaporation technique. For the developed particles, size, drug loading, entrapment efficiency, and surface morphology were determined. Further, the particles were suspended into bigel developed from oleogel and hydrogel (40:60) and assessed for stability, in vitro drug release, ex vivo skin permeation, retention, and in vivo study in BALB c mice for antipsoriatic potential. PLGA microparticles developed by solvent evaporation were found to have a mean particle size of 19.45 ± 1.74 μm. Drug loading and entrapment efficiency for clobetasol were found to be 43.5 ± 4.94% and 94.5 ± 3.68%, respectively. For the developed bigel, sustained in vitro drug release was observed till 7 h. Ex vivo skin permeation with the developed formulation was found to be higher than the marketed formulation and drug suspended in bigel. A retention study performed on pig skin suggested the topical skin retention of the drug. Further, the psoriatic model was developed in BALB c mice with IMQ cream, and it was observed that the developed formulation helped considerably reduce the irritation score and PASI scoring in mice as compared to the standard treatment. The same is corroborated with the help of histopathological studies performed by Hematoxylin and Eosin (H&E) staining in the same animals. The study findings suggest that clobetasol microparticle-loaded bigel formulation appeared to be a promising therapy option for psoriasis. [ABSTRACT FROM AUTHOR]