Search

Clobetasol propionate (CP) is a potent corticosteroid used for skin conditions but often causes side effects due its systemic absorption. To improve its solubility and reduce it side effects (like skin irritation, skin atrophy, hypopigmentation and steroidal acne), Microsponge (Msg) has been employed as a unique three-dimensional particle that can encapsulate hydrophilic and lipophilic drugs. This study aims to develop and evaluate CP Msg-loaded hydrogels. Two Clobetasol-loaded ethylcellulose-based Msg formulas were prepared using the quasi-emulsion solvent diffusion method, then they were incorporated into Carbopol hydrogel. Two ratios of Carbopol 940 (1% and 1.5% w/w) were used. The prepared hydrogel were assessed for appearance, pH, drug content, spreadability, extrudability, rheology, and in vitro release. The optimum hydrogel was compared to generic CP cream available locally and plain hydrogel. The results showed that both Msg formulas had good product yield, entrapment efficiency and highly porous micron size. The four prepared hydrogels revealed acceptable characterization including; pH ranged between 5.6and 6, drug content (98.8-100%) and % extrudability (80.7-92%) with pseudoplastic flow type. The hydrogel formula (F2Ha 1%) containing (1:1 weight ratio of CP: ethylcellulose) with (1%w\w Carbopol) was chosen as the optimized formula since it showed the highest spreadablility and approximately 43% of CP was released at 8 hours. The ex-vivo data including; the highest deposition in stratum corneum and epidermal/dermis with the flux, permeability coefficient and lag time of F2Ha were low, compared to plain hydrogel and marketed cream. Based on the study's finding, we concluded that CP Msg-loaded Carbopol hydrogel is a proper drug delivery system for topical application with minimized systemic absorption. [ABSTRACT FROM AUTHOR]

In this paper, the structure and properties of interpolymer complexes (IPC) based on sodium carboxymethylcellulose with a linear carbopol were studied. Interpolymer complexes were obtained by mixing aqueous solutions of Na-CMC and carbopol components in various ratios of components and pH of the medium. The structure of the obtained products was determined using the methods of IR spectroscopy and X–ray diffraction analysis. IR spectra in the range of 400-4000 cm-1 were recorded on spectrophotometers "NIKOLET Magna-560 IR" and "Specord–75 IR" (Karl Zeiss, GDR). X-ray diffraction analysis of IPС films was carried out on a Rigaku X-Ray installation with an X-ray generator with a rotating copper anode, at a voltage of 40 kV, with a current strength of 15 mA and using characteristic Cu-Ka radiation in the area of angles 0

Gelatin‐methacryloyl (GelMA) hydrogel has gained huge success in the last decades thanks to its versatilities in many applications. Notably, one of them is 3D bioprinting, as GelMA physical‐mechanical properties and biocompatibility of uncured formulation perfectly suit the requirements of a bioink. Nevertheless, before the photopolymerization, the hydrogel shows weak mechanical properties and long recovery time after stress application, which results in the inability to obtain complex and self‐standing forms due to structure collapse. In this work, Carbopol ETD 2020 NF, dissolved in cell culture medium, was used as supporting bath to optimize GelMA bioprinting and overcome its stability limitations. The achieved results demonstrated the possibility of printing shapes containing hollows with lumens or non‐planar surfaces, also by using nozzles with larger inner diameter, which reduced cell death during printing process, but were usually avoid because of low resolution. Moreover, constructs' extraction was easier when Carbopol solution was prepared in culture medium rather than in water, reducing sample handling. In conclusion, thanks to this supporting bath, it was possible to print cellularized scaffold, with channels that were then seeded, obtaining inner structure. Further, this Carbopol formulation could be considered an eligible candidate as a supporting bath to obtain GelMA 3D self‐standing‐shaped and vascularized scaffold. [ABSTRACT FROM AUTHOR]

The influence of apparent slip on oscillatory shear measurements of a viscoplastic microgel [0.6 wt. % of poly(acrylic acid)] is analyzed by Couette and parallel-plate rheometry and particle image velocimetry (Rheo-PIV). We first provide direct evidence of a critical shear stress for the onset of slip of the microgel under oscillatory (σos) and nonoscillatory measurements (σs). Afterward, we describe the effect of slip on oscillatory measurements via waveforms, Bowditch–Lissajous curves, Fourier transform (FT) rheology, PIV, and as a sequence of physical processes (SPP). The effect of slip is mainly observed at low oscillating frequencies. For amplitudes of the oscillating stresses σ0 ≤ σos, the microgel exhibits linear viscoelastic behavior with in-phase strain response. For σos< σ0 ≤ yield stress (σy), slip introduces a phase shift in the strain response with a forward-tilted waveform and "mango" shape Bowditch–Lissajous curves. Meanwhile, FT rheology shows negligible even harmonics. The strain measured by the rheometer does not match the true strain determined by PIV in the presence of slip, resulting in waveforms that depend on how the displacement distribution is interpreted. This result indicates a break in the symmetry of the flow, that is, the microgel response no longer follows the imposed oscillation, which makes any attempt to correct oscillatory data for slip complex. This behavior arises from recoil of the slipping microgel after reaching its maximum displacement in a cycle. Finally, we provide an overall picture of the kinematics of the process of yielding in the presence of slip as an SPP. [ABSTRACT FROM AUTHOR]

Sealing of soft tissues prevents leakage of gas and liquid, closes wounds, and promotes healing and is, therefore, of great significance in the clinical and medical fields. Although various formulations have been developed for reliable sealing of soft tissue, tradeoffs between adhesive properties, degradation profile, and tissue toxicity limit their clinical use. Hydrogel‐based adhesives, for example, are highly biocompatible but adhere very weakly to the tissue and degrade quickly, while oxidized cellulose patches are poorly absorbed and may cause healing complications postoperatively. Here, we present a novel strategy for tissue sealing based on bioadhesive microneedle patches that can spontaneously adhere to tissue surface through electrostatic interactions and swell within it. A series of microneedle patches made of pullulan, chitosan, Carbopol, poly (lactic‐co‐glycolic acid), and a Carbopol/chitosan combination were fabricated and characterized for their use in tissue sealing. The effect of microneedle composition on the fabrication process, physical and mechanical properties, in vitro cytotoxicity, and in vivo biocompatibility were examined. The needle structure enables microneedles to strongly fix onto various tissues via physical interlocking, while their adhesive properties improve staying time and sealing capabilities. The microneedle patch comprising Carbopol needles and chitosan as a second pedestal layer presented the best results in terms of sealing and adhesion, a consequence of the needle's swelling and adhesion features combined with the supportive chitosan base layer. Finally, single Carbopol/chitosan patches stopped intense liver bleeding in a rat model significantly quicker and with less blood loss compared with commercial oxidized cellulose patches. These microneedles can be considered a promising cost‐effective platform for adhering and sealing tissues as they can be applied quickly and painlessly, and require less trained medical staff and equipment. [ABSTRACT FROM AUTHOR]

Magrain is a depleting disease that sometimes requires extensive treatment, ideally with medication that targets the brain, with minimized systemic adverse effects, preferably with a single daily medication; these properties are offered partially by the current dosage form of Frovatriptan. formulation of Frovatriptan binary ethosome into mucoadhesive nasal in situ gel to extend the drug's residence time. The particle size was 154.1±4.38 nm of t eh Frovatriptan binary ethosome. In situ, gel formulas were prepared to utilize the cold technique, using 18%w/v poloxamer 407 with different concentrations of Carbopol 934 and the clarity, pH, Frovatriptan content spreadability, mucoadhesive force, in vitro diffusion via nasal mucosa and the optimal formula underwent further investigations. In-situ gel F2 (0.2% Carbopol) demonstrated the best spreadability of 12.88±0.186 cm2 /min, 99% drug content mucoadhesive strength of 645.32±0.054 dynes/cm2, percent release of 98.56±0.041 after 24 hours and permeability increased by around 3.68-fold compared to the pure drug and histopathologically showed favorable outcomes. Mucoadhesive Frovatriptan-binary ethosome-loaded nasal in situ gel is an effective method of treating migraines. [ABSTRACT FROM AUTHOR]

The objective of this study is Preparation and evaluation of gastro-retentive floating tablets of Ibandronic acid by direct compression method polymers or combination. In this study, Ibandronic acid, the most commonly used biphosphonate for treating osteoporosis, was formulated as gastro retentive dosage form (GRDF) tablets to enhance its oral bioavailability. GRDDs are an approach to prolong gastric residence time, there by targeting site-specific drug release in the upper GIT for local or systemic effect. GRDF tablets of Ibandronic acid (200 mg) were characterized with the effects of Carbopol 934P, HPMC 4KM and Na-CMC at various ratios on swelling, floating, physical integrity. A prolonged dissolution profile of Ibandronic acid GRDF tablets developed in this study was observed for its thickness, friability, hardness, drug content and in-vitro drug release. Formulated Floating tablets of Ibandronic acid gave satisfactory results for various physicochemical parameters like hardness, friability, thickness, weight variation and content uniformity. Sodium bicarbonate has predominant effect on the buoyancy lag time, while HPMC K4M has predominant effect on total floating time and drug release. From the study it is evident that a promising controlled release floating tablets of Ibandronic acid can be developed to increase gastric residence time and thereby increasing its bioavailability. Both doses significantly reduced the occurrence risk of new vertebral fractures by 50–52 percent when compared to the effects of the placebo drug. [ABSTRACT FROM AUTHOR]

In this paper, the structure and properties of interpolymer complexes (IPC) based on sodium carboxymethylcellulose with a linear carbopol were studied. Interpolymer complexes were obtained by mixing aqueous solutions of Na-CMC and carbopol components in various ratios of components and pH of the medium. The structure of the obtained products was determined using the methods of IR spectroscopy and X-ray diffraction analysis. IR spectra in the range of 400-4000 cm-1 were recorded on spectrophotometers "NIKOLET Magna-560 IR" and "Specord-75 IR" (Karl Zeiss, GDR). X-ray diffraction analysis of IPС films was carried out on a Rigaku X-Ray installation with an X-ray generator with a rotating copper anode, at a voltage of 40 kV, with a current strength of 15 mA and using characteristic Cu-Ka radiation in the area of angles 0 <2θ <40. IR spectroscopic data show that the interpolymer complexes based on Na-CMC and carbopol obtained in moderately acidic regions are stabilized due to the cooperative hydrogen bond between the carboxyl groups of Na-CMC and the carbonyl groups of carbopol. X-ray diffraction analysis has shown that a change in the composition of the interpolymer complex leads to a change in the structure, which depends on the structure and nature of the interchain bonds. It is ascertained that an increase in the number of hydrogen bonds leads to a more ordered state of the resulting interpolymer complex. It is revealed that the formation of an interpolymer complex due to hydrogen bonds provides additional stability. This can serve as one of the means of controlling the structure and properties of the IPC of sodium carboxymethylcellulose with carbopol. [ABSTRACT FROM AUTHOR]

A novel approach was devised to address the challenges in delivering cisplatin (CIS) for lung cancer treatment. This involved the development of a non-invasive hydrogel delivery system, aiming to minimize side effects associated with its administration. Using carbopol 971 (CP) and chitosan (CH) at varying ratios, the hydrogels were prepared and loaded with eco-friendly iron oxide nanoparticles (IONPs) conjugated to CIS. The physical properties, yield, drug loading, and cytotoxicity against lung cancer cell lines (A549) were assessed, along with hydrogel rheological properties and in vitro drug diffusion. Hydrogel A1 that composed of 1:1 of CP:CH hydrogel loaded with 100 mg IONPs and 250 µg CIS demonstrated distinctive properties that indicate its suitability for potential delivery. The loaded greenly synthesized IONPs@CIS exhibited a particle size of 23.0 nm, polydispersity index of 0.47, yield of 71.6%, with 88.28% drug loading. They displayed significant cytotoxicity (61.7%) against lung cancer cell lines (A549), surpassing free CIS cytotoxicity (28.1%). Moreover, they demonstrated shear-thinning behaviour, viscoelastic properties, and Fickian drug release profile over 24 h (flux 2.34 µg/cm2/h, and permeability 0.31 cm/h). [ABSTRACT FROM AUTHOR]

To develop a new kind of famotidine-resin microcapsule for gastric adhesion sustained release by screening out suitable excipients and designing reasonable prescriptions to improve patient drug activities to achieve the expected therapeutic effect. The famotidine drug resin was prepared using the water bath method with carbomer 934 used as coating material. Microcapsules were prepared using the emulsified solvent coating method and appropriate excipients were used to prepare famotidine sustained release suspension. Pharmacokinetics of the developed microcapsules were studied in the gastrointestinal tract of rats. The self-made sustained-release suspension of famotidine hydrochloride effectively reduced the blood concentration and prolonged the action time. The relative bioavailability of the self-made suspension of the famotidine hydrochloride to the commercially available famotidine hydrochloride was 146.44%, with an average retention time of about 5h longer, which indicated that the new suspension had acceptable adhesion properties. The findings showed that the newly developed famotidine-resin microcapsule increased the bioavailability of the drug with a significant sustained-release property. [ABSTRACT FROM AUTHOR]

Green tea extract has many potent antioxidants known for their beneficial health effects. One such compound is epigallocatechin-3-gallate, which exhibits chemotherapeutic properties and can reduce cholesterol levels in blood. Since the topical delivery of drugs is difficult, nanogels have great potential due to their reduced particle size and structural properties. The present study investigated the impact of independent variables such as carbopol and triethanolamine (TEA) concentrations on nanogel pH, viscosity, and in vitro diffusion. All formulations were generated by Box-Behnken design and followed the nanoprecipitation technique to prepare nanogel. Formulations were tested for pH, homogeneity, spreadability, viscosity, drug content, particle size, zeta potential, and entrapment efficiency (EE) and characterized for surface morphology. The prepared chitosan nanoparticle designated F5 was seen to show an encapsulation efficiency of 94.11% with a practical yield of 94.41%. Also, after GTE loading, the nanogel formulation NG15 showed optimal drug content of 99.87%. Besides, the nanogel was also characterized based on F5 showing the best results. From surface plots, the varying effects of interacting parameters could be elucidated, and ANOVA studies showed that all designed models were significant with acceptable values for the statistical parameters. Conclusively, GTE-loaded nanogel seems to be robust and therefore could be used with a promising potential for topical drug delivery. [ABSTRACT FROM AUTHOR]

Ophthalmic films are the best sustained-release ocular drug delivery system. The present study targets developing such ocular films of antibacterial with corticosteroid and evaluating its potential. Conventional ocular dosage forms have low bioavailability with low therapeutic response. The solvent cast method employed in ophthalmic films has triggered the minds of researchers to design sustained drug delivery systems overcoming pre-corneal constraints. The compatibility of antibacterial with Loteprednol Etabonate added polymers, excipients were evaluated through preformulation studies. Different combinations of ocular inserts with antibacterial drug and corticosteroid, excipients were formulated and evaluated. Formula CLE 80 (Ciprofloxacin Hydrochloride with Loteprednol Etabonate) fulfilled the needs of all organoleptic parameters like appearance, texture, surface pH, drug content, and in-vitro studies. The results predicted CLE 80 ophthalmic film would be a promising controlled-release formulation for better patient compliance. [ABSTRACT FROM AUTHOR]

Abstract Sealing of soft tissues prevents leakage of gas and liquid, closes wounds, and promotes healing and is, therefore, of great significance in the clinical and medical fields. Although various formulations have been developed for reliable sealing of soft tissue, tradeoffs between adhesive properties, degradation profile, and tissue toxicity limit their clinical use. Hydrogel‐based adhesives, for example, are highly biocompatible but adhere very weakly to the tissue and degrade quickly, while oxidized cellulose patches are poorly absorbed and may cause healing complications postoperatively. Here, we present a novel strategy for tissue sealing based on bioadhesive microneedle patches that can spontaneously adhere to tissue surface through electrostatic interactions and swell within it. A series of microneedle patches made of pullulan, chitosan, Carbopol, poly (lactic‐co‐glycolic acid), and a Carbopol/chitosan combination were fabricated and characterized for their use in tissue sealing. The effect of microneedle composition on the fabrication process, physical and mechanical properties, in vitro cytotoxicity, and in vivo biocompatibility were examined. The needle structure enables microneedles to strongly fix onto various tissues via physical interlocking, while their adhesive properties improve staying time and sealing capabilities. The microneedle patch comprising Carbopol needles and chitosan as a second pedestal layer presented the best results in terms of sealing and adhesion, a consequence of the needle's swelling and adhesion features combined with the supportive chitosan base layer. Finally, single Carbopol/chitosan patches stopped intense liver bleeding in a rat model significantly quicker and with less blood loss compared with commercial oxidized cellulose patches. These microneedles can be considered a promising cost‐effective platform for adhering and sealing tissues as they can be applied quickly and painlessly, and require less trained medical staff and equipment.

For the study, mucoadhesive buccal tablets containing Meclizine Hydrochloride (MCZ HCL) were designed to avoid first-pass metabolism and enhance its bioavailability while reducing the dose administration frequency. As a result, this work aimed to design, evaluate, and determine the optimum conditions for the bioadhesion and drug release. MCZ HCL mucoadhesive buccal tablets were prepared using multiple grades of HPMC, including HPMC 15 cps, 50 cps, 100 cps, and HPMC K4M, by the direct compression method. Ethyl cellulose was employed as a backing layer to facilitate the unidirectional flow of medication in the buccal region of the mouth. Using the central composite design (CCD), the drug delivery formulations undergo a thorough optimization process. The response surface and contour plots were generated, and grid searches and feasibility analyses were conducted to select the most effective formulations. The developed formulations underwent various tests to determine their physiochemical characteristics and in-vitro drug release. Optimized formulation containing HPMC 15 cps 24.63 mg and Carbopol 934P 4.17 mg showed t50 in 5.6 h. Additionally, the optimized formulation's mucoadhesive strength was 7.04 ± 0.41, and its swelling index was 99.82% after 8 h. Furthermore, studies conducted with FTIR spectroscopy revealed no interactions between the drug and the excipient. According to short-term stability experiments performed on the promising formulation, there were no significant changes in the amount of drug present.

Objectives: The existing study is concerned with the formulation and optimization of dextromethorphan hydrobromide floating tablets via central composite design. Materials and Methods: Direct compression method was employed to prepare the tablets. Drug-excipient studies were executed through FT-IR and DSC analysis. The independent variables selected were the concentrations of Carbopol 934 (X1) and HPMC K15M (X2). The dependent variables designated were Floating Lag Time (FLT) and Drug Release (DR) at 12 hr. The model was found to be nonlinear and the curvature effect was significant. Hence, the system suggested to central composite design. Results: FT-IR studies demonstrated that there is no considerable interaction amid the drug and the excipients. DSC studies revealed that drug and excipient were compatible as there is no significant alteration in melting point of drug when blended with excipients. The precompression parameters of the formulations showed good flow properties. The evaluation of post compression parameters indicated that all the prepared formulations were within the specified limits. Floating lag time of formulations were marked to be less than 1 min and total floating time exceeding 12 hr. Percentage drug release of all formulations were in the range of 89.7% to 99.4%. The obtained design space/contour plots were used for selecting batches in desirable ranges. Conclusion: The results revealed that experimental design was successfully used to optimize polymer concentrations. It was determined that the central composite design would be used to formulate dextromethorphan gastroretentive floating tablets with fewer trials and higher quality features. [ABSTRACT FROM AUTHOR]

Objectives: The aim of the study was to design, develop, and optimize the buccal tablets containing extract of Terminalia chebula Retz. for the treatment of asthma. Materials and Methods: Buccal tablets were made using the direct compression method, and screening tests with various polymers were run to see how they affected the properties of the tablets. The utilisation of response surface methods, two polymer types, carbopol® and HPMC, were chosen for additional optimization research. Strength of mucoadhesion and % two significant responses that the drug permeated after 8 hr from the buccal mucosa were chosen. By using a swelling index analysis, the profiles and kinetics of in vitro drug release were examined. Results: The Terminalia chebula Retz. content in buccal tablets was determined to be 99.14±0.44%, and a DSC analysis showed that there was no chemical interaction between the ingredients of the tablet (8 g carbopol 934 and 20 g HPMC K15 made up the optimal formulation). After 8 hr of in vitro dissolving studies, a cumulative Terminalia chebula Retz. release of 90% was reached, which was confirmed by swelling analysis. Conclusion: The findings suggested that Terminalia chebula Retz's. optimised buccal tablets would be a promising and different delivery method for the treatment of asthma. [ABSTRACT FROM AUTHOR]

ABSTRACTDamage to body tissue either deeply or superficially causes pain sensation in response to which Inflammation occurs which is a normal protective natural response of the body to a variety of hostile agents. Different treatment options, including conventional and herbal therapies, are available for pain and inflammation. This study was designed to evaluate the polyherbal n-hexane and methanolic extracts and their hydrogel formulations prepared from commonly available medicinal plants for their analgesic and anti-inflammatory potential. Cinnamomum verum J. (bark), Moringa oleifera L. (leaves), Nigella sativa L. (seed), and Trigonella foenum graecum L. (seed) were collected and purchased from the vicinity and local market of Multan Punjab, Pakistan. After drying, extraction was carried out by maceration separately with two different solvents (methanol and n-hexane). An equal quantity of all methanolic and n-hexane extracts was used to formulate polyherbal methanolic and n-hexane extracts separately. Then 1%, 3%, and 5% pH-based hydrogel formulations of methanolic and n-hexane polyherbal extract were prepared. All prepared six formulations were evaluated for pH, rheological study, spreadability, extrudability, stability study, texture, color, and for toxicological study. Then analgesic and anti-inflammatory potential of methanol and n-Hexane polyherbal extracts at (200, 400 and 800.0 mg/kg) in comparison with diclofenac sodium (100 mg/kg) and prepared gel formulations (1%, 3%, and 5%) were also evaluated in comparison to diclofenac sodium 1% gel (standard drug). Both polyherbal extracts and their gel formulations have significant analgesic and anti-inflammatory potential but methanolic extract and its hydrogel have slightly more potential as compared to n-hexane extracts and its prepared hydrogel. Results also revealed that their gel formulations have more significant analgesic and anti-inflammatory potentials as compared to extracts. All pH-based gels have good texture, spreadability, extrudability, stability, and are safe to use. It is concluded that methanolic polyherbal extract and hydrogel prepared from methanolic extract have more analgesic and anti-inflammatory potential as compare to n-Hexane extract and hydrogel prepare from n-Hexane extract.

Keeping in view the progressive future prospectus of carbohydrate research, herein, the potential of bioactive polysaccharides aloe vera (AV) and sterculia gum (SG) was explored to develop network hydrogel wound dressings. Both polysaccharides, acemannan of AV gel and glucuronic-galacturonic acid of SG accelerate wound healing process. The antibiotic drug cefuroxime encapsulated dressings were designed by graft-copolymerization with carbopol. The copolymers were characterized by SEM, AFM, FTIR, C13 NMR, XRD, TGA-DTG, DSC and swelling studies. The slow diffusion of cefuroxime drug exhibited non-Fickian mechanism and release of drug was occurred with a first order kinetic model. Polymer-bio membrane interactions indicated mucoadhesion nature. The clot formation was reduced during polymer-blood interactions indicated bio-compatible nature of the dressings moreover dressings were found antioxidant in nature. The porous dressings were O2 permeable and microbial impermeable. The hydrogel dressings revealed antimicrobial activity against P. aeruginosa. Degree of antimicrobial activity enhanced in case of hydrogel wound dressings loaded with cefuroxime. Overall, the results of these biochemical assays, sustained release of antibiotic drug and inherent wound healing potential of AV-SG indicated the use of hydrogels as dressing materials for better wound healing.

Landslide-generated waves occur as a result of the intrusion of landslides such as mud flows and debris flows into bodies of water such as lakes and reservoirs. The objective of this study was to determine how the momentum is transferred from the sliding mass to the body of water on the basis of theoretical analysis and physical model experiments. Considering the viscoplastic idealization of natural landslides, the theoretical model was established based on the momentum and mass conservation of a two-phase flow in a control volume. To close the theoretical equations, slide thickness and velocity passing through the left boundary of the control volume were estimated by lubrication theory, and the interaction forces between the slide phase and water phase, including hydrostatic force and drag force, were given by semiempirical equations fitted with experimental data obtained using the particle image velocimetry (PIV) technique. The near-field velocity fields of both the sliding mass and the body of water, as well as the air–water–slide interfaces, were determined from the experiments. The theoretical model was validated by comparing the theoretical and experimental data of the slide thickness and slide velocity, as well as the momentum variations of the two phases in the control volume. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Faculty of Pharmacy of Ankara University / Ankara Üniversitesi Eczacilik Fakültesi Dergisi is the property of Ankara University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: Resistance to antimicrobial drugs as a result of prolonged use usually results in clinical failure, especially in wound infections. Development of effective antimicrobial therapeutics for the management of infected wounds from a natural source with improved therapeutic effects is a pressing need. Objective: In this study, carbopol-mastic gum-based topical gels were loaded with silver nanoparticles in combination with either neem bark extract or carvacrol oil. The effect of combining silver nanoparticles with neem bark extract or the essential oil carvacrol in the prepared gel formulations was investigated on selected bacterial strains. Method: The prepared gels were characterised by Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM) and ultraviolet--visible (UV--vis) spectroscopy, followed by antimicrobial analysis against selected strains of bacteria. Results: There was no interaction between the loaded natural extract or essential oil and the polymer used for the preparation of the formulations, which was visible from the FTIR spectra of the formulations. The gels were selective and effective against selected strains of bacteria. However, the combination of the silver nanoparticles with essential oil or natural extract in some of the gel formulations rendered the formulation ineffective against some of the bacterial strains. Conclusion: The gel formulations were effective against bacterial strains such as Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalis which are the common causes of wound infections. Incorporation of silver nanoparticles into the topical formulations with natural extracts is usually a good approach to overcome antibiotic-resistant infections. However, the combination of antibacterial agents must be managed carefully. [ABSTRACT FROM AUTHOR]

Herein, we propose an oxygen nanobubbles-embedded hydrogel (ONB-G) with carbopol for oxygenation of wounds to accelerate the wound healing process. We integrate carbopol, hydrogel, and dextran-based oxygen nanobubbles (ONBs) to prepare ONB-G where ONBs can hold and release oxygen to accelerate wound healing. Oxygen release tests showed that the proposed ONB-G could encapsulate oxygen in the hydrogels for up to 34 days; meanwhile, fluorescence studies indicated that the ONB-G could maintain high oxygen levels for up to 4 weeks. The effect of carbopol concentration on the oxygen release capacity and rheological features of the ONB-G were also investigated along with the sterility of ONB-G. HDFa cell-based studies were first conducted to evaluate the viability, proliferation, and revival of cells in hypoxia. Scratch assay and mRNA expression studies indicated the potential benefit for wound closure. Histological evaluation of tissues with a pig model with incision and punch wounds showed that treatment with ONB-G exhibited improved healing compared with hydrogel without ONBs or treated without the gel. Our studies show that dextran-shell ONBs embedded in a gel (ONB-G) have the potential to accelerate wound healing, given its oxygen-holding capacity and release properties. [ABSTRACT FROM AUTHOR]

The vane-in-cup (VIC) geometry has been widely used for the rheological characterization of yield-stress fluids because it minimizes slip effects at the liquid/solid interface of the rotating geometry and reduces sample damage during the loading process. However, severe kinematic limitations arising from the spatial complexity of mixed shear and extensional flow have been identified for quantitative rheometrical measurements in complex fluids. Recently, vanes with fractal cross sections have been suggested as alternatives for accurate rheometry of elastoviscoplastic fluids. In this work, the steady fractal vane-in-cup (fVIC) flow of a Newtonian fluid and a nonthixotropic Carbopol® 940 microgel as well as the unsteady flow of a thixotropic κ-Carrageenan gel are analyzed using rheo-particle image velocimetry (Rheo-PIV). We describe the velocity distributions in all cases and show that the fVIC produces an almost axisymmetric flow field and rotation rate-independent "effective radius" when used with both the Newtonian fluid and the microgel. These findings are supported by 2D simulation results and enable the safe use of both the Couette analogy and the torque-to-stress conversion scheme for a 24-arm fVIC as well as validate it as a reliable rheometrical tool for characterization of a variety of complex fluids. With the κ-Carrageenan gel, however, axial shearing/compression while inserting the rheometric tool into the sample also accelerates syneresis that ultimately results in shear banding for Couette and fVIC flows. By comparing results obtained using the 24-arm fVIC with other conventional geometries, we investigate the effect that the lateral and cross-sectional (shearing/compressing) area of the measuring fixture have on disrupting the κ-Carrageenan gel during its insertion. [ABSTRACT FROM AUTHOR]

Providing an appropriate treatment to accelerate wound healing after a burn is a challenging problem. Therefore, finding advanced and cost-effective products reducing the recovery time is essential. This study aimed to introduce a simple strategy for the preparation of a multifunctional dressing bearing natural-based materials for the treatment of burn wounds. Carbopol (Carb) gel was loaded with carnosine-enriched bentonite (CEB), and the wound healing potential was evaluated using a rat burn wound model. The acceptable physicochemical properties of Carb-CEB gel provided an appropriate media for improved fibroblast cell adhesion, migration, survival, and growth compared to the Carb gel alone. Furthermore, ferric reducing antioxidant potential (FRAP) assay revealed superior antioxidant activity of Carb-CEB than Carb (*P ≤ 0.05). Macroscopically, the wound healing rates of Carb and Carb-CEB were approximately 84 and 95%, respectively, confirming the significant role of CEB in accelerating the wound closure. Histological evaluation also showed better epithelialization, angiogenesis, and reduction in inflammatory cells in the rats treated with Carb-CEB compared to the controls. In Carb-CEB-treated wounds, the regenerated epidermis was thicker and the number of blood vessels increased significantly. Overall, in vitro and in vivo studies suggested that Carb-CEB could be introduced as a promising wound dressing for further study of wound healing. [ABSTRACT FROM AUTHOR]

Copyright of Detergent & Cosmetics is the property of Detergent & Cosmetics Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The bacterial infections are very common and become a serious issue like in case of infections of one and more reproductive organ, inflammation on protective membrane of brain and spinal cord, inflammation of lungs air sacs, body drainage system infections, problem in body’s extreme response and infection caused by sexually transmitted bacteria in male and female. Generally, these bacterial infections are treated by using antibiotics like cefotaxime that is a semisynthetic, β-lactamase resistant, third-generation broad-spectrum cephalosporin. The common side effects of cefotaxime are uneasiness of stomach before vomiting, sneezing, itching. The topical antibacterial dosage forms like creams, gel, and ointment have some demerits and low duration of drug release. The emulgel is an alternative for topical drug delivery with several merits like enhanced skin penetration and improved bioavailability, reduced dosing, improved patient acceptability with targeted drug delivery, freedom of termination of the therapy at any time, drug delivery in controlled fashion for prolong duration. The aim of study was to develop a biphasic promising drug delivery system emulgel of cefotaxime. The 23 experimental design was used to prepare various emulgel batches to determinant the effect of liquid paraffin, span 20 and tween 20 on the performance of emulgel. The Batch F1 showed the maximum drug release while batch F8 up to 240 minutes. The drug release kinetics study of Batch F8 showed the Higuchi-Matrix as a best fit model and the Fickian Diffusion as a mechanism of drug release with R2 value 0.9158 and K value 8.4741.

Urticaria affects all age groups of a population. It is triggered by allergens in foods, insect bites, medications, and environmental conditions. Urticaria is characterized by itching, a burning sensation, wheals and flares, erythema, and localized edema. The aim of this study was to develop a polymeric dosage form of ebastine using Carbopol 940 and mixture of span and tween. The emulsion was prepared, the gelling agent was added and the desired emulgel loaded with active drug was formulated. The formulations were subjected to physical stability, pH, viscosity, spreadability, drug content analysis, thermal analysis, in vitro drug release, and in vivo anti-allergic activity in animal model. The formulated emulgel exhibited good physical stability. The pH of the formulation was in the range of 5.2 ± 0.17 to 5.5 ± 0.20 which is suitable for topical application. Insignificant changes (p > .05) were observed in viscosity and spreadability of stored emulgels. The drug content was in the official limit of Pharmacopeia (i.e. 100 ± 10%). DSC measurements predicted that there is no interaction between the active moiety and excipients in emulgel formulation. The optimized formulation (ES3) released 74.25 ± 1.8% of ebastine after 12 h. The ebastine emulgel showed significant (p

The objective of the current research to investigate the transdermal delivery of phytosomal Manjistha extract gel (MJE gel). The optimized formulation was prepared and evaluated for different parameters. MJE-loaded phytosomes were prepared by solvent evaporation method using rotary evaporator. The formulation was prepared with a variable concentration of lecithin (0.15–0.25% w/v), with stirring speed of the round bottom flask (80–160 rpm). Design expert software was used for the optimization of MJE-loaded phytosomal formulations. Central composite design-based factorial design was applied and evaluated for vesicular size and entrapment efficiency as dependent variables. The optimized formulation was further characterized with vesicle size, zeta potential, in vitro release. The Carbopol 934 was used to convert the phytosomal formulation (F10) into phytosomal gel and evaluated for ex vivo permeation to check the difference in permeation profile in compare to conventional MJE gel. The optimized MJE-loaded phytosomal formulation (F10) showed the vesicular size of 122.15 ± 3.73 nm, entrapment efficiency of 96.25 ± 2.45% with PDI value of 0.98 ± 0.06. Among the drug release kinetic models, the formulation followed the Higuchi model with drug release of 84.2 ± 4.1% in 12 h. Transmission electron micrograph showed the uniform structure and spherical shape. The prepared phytosomal gel shows prolonged release and enhanced permeation compared to conventional MJE gel. [ABSTRACT FROM AUTHOR]

The study was aimed at developing topical gel containing papain as the drug and assessing its antipsoriatic activity. Carbopol was used as the polymer and drug-excipient compatibility was ascertained by infrared spectroscopy (Fourier transform) and differential scanning calorimetry. All prepared formulations were evaluated for viscosity, pH, homogeneity, extrudability, spreadability, in vitro diffusion and release kinetics. Anti-proliferative activity was determined on HaCaT cell line. The optimized formulation, F2 exhibited pH 6.8, optimum viscosity, extrudability and spreadability for convenient use. The optimized formulation followed Higuchi kinetic model with release mechanism being super-case two transport. The anti-proliferative activity of optimized formulation on HaCaT cell line showed only 3.9 % cells to be viable with respect to control confirming its efficacy in treating psoriasis. The gel exhibited stability under accelerated stability conditions. It can be inferred from the study that papain gel can be effectively used for managing psoriasis and its single application would give prolonged action. [ABSTRACT FROM AUTHOR]

The hands are one of the most susceptible parts of the human body to bacterial infection. One way to maintain health is to maintain hand hygiene. Ethanolic rambutan rind extract from Aceh province has been studied in order to determine if it can inhibit bacterial growth. This research was conducted to determine the antiseptic activity of the ethanol extract of rambutan rind against Stahpylococcus aureus by determining the phenol coefficient and determining whether the ethanolic extract of Aceh's rambutan rind can be formulated into a hand sanitizer gel. Antiseptic activity testing was performed using the Rideal-Walker method which was carried out in 5 dilutions (1:100, 1:150, 1:200, 1:250 and 1:300). The absorbance measurement showed that the extract could act as an antiseptic, at a concentration of 1% and at a dilution of 1:200 which has phenol coefficient of 1.67. The ethanolic extract of Aceh's rambutan rind can be formulated in the form of a hand sanitizer gel using 1% Carbopol as gelling agent. The results showed that the gel was brown with a distinctive menthol odor and changed into a dark brown color after a cycling test. The evaluation results of all formulas appropriated the requirements except for adhesion parameter. The results of the irritation test showed that the volunteers did not experience any signs of irritation. The results of the preference test showed that the respondents liked the shape and aroma parameters but not the color parameter. [ABSTRACT FROM AUTHOR]

Retinoids are considered the mainstay treatment for moderate to severe acne. Adapalene, a third-generation retinoid, has physiochemical properties which hinder the effective delivery of the drug to the skin. Therefore, the current study aimed to develop and evaluate adapalene liposomal loaded gel (ADA-LP gel) for the effective management of acne to improve tolerability and delivery to targeted sites as compared to the conventional dosage form of the drug. A novel spontaneous phase transition method (SPT) was used to formulate liposomes. Liposomal formulation (ADA-LP) was prepared and optimized based on particle size, zeta potential, and PDI. Optimized formulation was further characterized by different techniques and loaded into Carbopol gel. In vitro drug release, ex vivo permeation, and in vivo studies were performed using the prepared adapalene-loaded liposomal-based gel. The in vivo study was done employing the testosterone-induced acne model in mice. The optimized formulation had a size of 181 nm, PDI 0.145, and a zeta potential of −35 mV, indicating that the formulation was stable. Encapsulation efficiency was 89.69 ± 0.5%. ADA-LPs were loaded into the gel. Prepared ADA-LP showed a 79 ± 0.02% release of drug in a sustained manner, within 24 h. The ex vivo permeability study showed a total of 43 ± 0.06 µg/cm2 of drug able to permeate through the skin within 24 h. Moreover, only 28.27 ± 0.04% was retained on the epidermis. The developed ADA-LP gel showed significant improvement in the acne lesions in mice with no visible scars and inflammation on the skin. Therefore, ADA-LP-based gel could be a promising carrier system for the safe and effective delivery of Adapalene. [ABSTRACT FROM AUTHOR]

Background: Tretinoin (TRE) is, for its anti-comedogenic and comedolytic activity, widely used in the topical treatment of acne vulgaris. The effect lies in the regulation of sebum production and collagen synthesis. The study is devoted to the formulation of dermal gels containing TRE using microemulsion as the drug solubilizer. Methods: The aim was to evaluate the effect of the reference microemulsion (ME) and lecithin-containing microemulsion (MEL) on the release of TRE through the synthetic membrane (in vitro) and the pig's ear skin (ex vivo) through the Franz cell diffusion method. Subsequently, after an ex vivo study, the amount of the drug in the skin influenced by the applied formulation was determined. In addition, the impact of ME on the microscopic structure, texture, and rheological properties of gels was evaluated. Results: On the basis of the analysis of texture, rheological properties, and drug release studies, Carbopol formulations appear to be more appropriate and stable. Considering the synthetic membrane as a stratum corneum, the Carbopol gel penetrated about 2.5-higher amounts of TRE compared to the Xanthan gel. In turn, ex vivo studies suggest that MEL slows the drug transfer to the dissolution medium, simulating absorption into the blood, which is a desirable effect in local treatment. The drug retention study proved the highest amounts of TRE in the skin to which microemulsion-Carbopol formulations were applied. Conclusion: The results confirm the benefit of TRE solubilization in ME due to its bioavailability from the tested dermal formulations. [ABSTRACT FROM AUTHOR]

Damage to body tissue either deeply or superficially causes pain sensation in response to which Inflammation occurs which is a normal protective natural response of the body to a variety of hostile agents. Different treatment options, including conventional and herbal therapies, are available for pain and inflammation. This study was designed to evaluate the polyherbal n-hexane and methanolic extracts and their hydrogel formulations prepared from commonly available medicinal plants for their analgesic and anti-inflammatory potential. Cinnamomum verum J. (bark), Moringa oleifera L. (leaves), Nigella sativa L. (seed), and Trigonella foenum graecum L. (seed) were collected and purchased from the vicinity and local market of Multan Punjab, Pakistan. After drying, extraction was carried out by maceration separately with two different solvents (methanol and n-hexane). An equal quantity of all methanolic and n-hexane extracts was used to formulate polyherbal methanolic and n-hexane extracts separately. Then 1%, 3%, and 5% pH-based hydrogel formulations of methanolic and n-hexane polyherbal extract were prepared. All prepared six formulations were evaluated for pH, rheological study, spreadability, extrudability, stability study, texture, color, and for toxicological study. Then analgesic and anti-inflammatory potential of methanol and n-Hexane polyherbal extracts at (200, 400 and 800.0 mg/kg) in comparison with diclofenac sodium (100 mg/kg) and prepared gel formulations (1%, 3%, and 5%) were also evaluated in comparison to diclofenac sodium 1% gel (standard drug). Both polyherbal extracts and their gel formulations have significant analgesic and anti-inflammatory potential but methanolic extract and its hydrogel have slightly more potential as compared to n-hexane extracts and its prepared hydrogel. Results also revealed that their gel formulations have more significant analgesic and anti-inflammatory potentials as compared to extracts. All pH-based gels have good texture, spreadability, extrudability, stability, and are safe to use. It is concluded that methanolic polyherbal extract and hydrogel prepared from methanolic extract have more analgesic and anti-inflammatory potential as compare to n-Hexane extract and hydrogel prepare from n-Hexane extract. [ABSTRACT FROM AUTHOR]

The present study was designed to formulate a 5% topical gel formulation containing dexibuprofen. Herein, we reported the utilization of different gelling polymers including hydroxyl propyl methyl cellulose (HPMC), carboxy methyl cellulose (CMC), carbopol 940 and leutrol F127 at three concentration levels. Overall, twelve trials (TD1 to TD12) were prepared in four batches (DEX-I to DEX-IV), each having three trial dexibuprofen gel formulations. All formulations were evaluated for organoleptic properties, clarity, pH, consistency, viscosity and spreadability. Trials of DEX-I and DEX- III batches (containing HPMC and carbopol 940polymers respectively), were a lack in smoothness, clarity and viscosity. Contra wise, TD5, TD6 dexibuprofen gel formulations of batch DEX-II and TD10, TD11 and TD12 of DEX-IV having CMC and lutrol® F127 correspondingly were found to be viscous and free from grittiness and precipitation. In vitro drug kinetics revealed the Weibull kinetic model as the best (r2>0.999, AIC 31.427-37.381, MSC 2.259-3.421). Stability testing was performed on the selected formulations (TD5, TD6, TD10, TD11 and TD12) having acceptable physicochemical attributes. Only TD11 and TD12 were found to be stable at room temperature after three months. Based on the findings, it is concluded that lutrol® F127 based dexibuprofen gel formulations delivered excellent spreadability, better drug release, and satisfactory stability profile. [ABSTRACT FROM AUTHOR]

Hypothesis: Superabsorbent polymers are modifiers that have broad applications. One of their applications is in concrete production industry. The use of these materials for supplying water to cement materials and their curing process has attracted the attention of researchers. Using SAPs in concrete is a valuable tool for areas where conventional curing is very difficult, such as extreme weather conditions that can lead to excessive evaporation and freezing. It also saves water.Methods: Modified carbopol was prepared using poly(ethylene glycol) methyl ether methacrylate as a monomer with a molecular weight of 300 in amounts of 1, 2 and 3 g and with azobisisobutyronitrile (AIBN) as the initiator by ultrasound method. The properties of the prepared microgel and its effect on the properties of cement paste are investigated. The prepared microgel has been studied using FTIR analysis, scanning electron microscopy, particle size determination and swelling properties. In addition, the effect of prepared microgel on different properties of cement paste, such as rheology, compressive and flexural strength and hydration, is investigated.Findings: The results of FTIR and microscopic images showed that the monomer was modified. According to the swelling results, it was observed that carbopol has no absorption and it is dissolved. After modification, the swelling and absorption properties are obtained. The swelling capacity in water and saline solution has increased first and then decreased with increasing monomer concentration. The resultant cement pastes show that the compressive strength of samples is decreased in the presence of modified carbopol. In addition, the strength of the cement paste prepared with commercial superabsorbent (polyacrylic acid sodium salt) has increased with the same water:cement ratio. The flexural strength is reduced in all samples compared to the reference. According to the results, the modified carbopol has increased the viscosity of the cement pastes. According to the XRD results, hydration and curing of samples with superabsorbent have completed within 28 days compared to the control cement. Therefore, it can be concluded that superabsorbents generally cause a delay in hydration, and besides the hydration of the superabsorbent-cement specimens is decreased by reducing the monomer.

Tayyba Saher,1 Rizwana Manzoor,1 Khizar Abbas,1 Jahanzeb Mudassir,2 M Asif Wazir,3 Ejaz Ali,4 Faheem Ahmad Siddique,5 Akhtar Rasul,6 Muhammad Imran Qadir,7 Ambreen Aleem,8 Naeem Qaiser,9 Adeel Usman,3 Muhammad Romman,10 Muhammad Sajid Ali11 1Department of Pharmacognosy, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan; 2Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan; 3Department of Pharmacognosy, Faculty of Pharmacy and Pharmaceutical sciences,University of Karachi, Karachi, Pakistan; 4University College of Pharmacy, University of Punjab, Lahore, Pakistan; 5Department of Pharmacy, University of Central Punjab, Lahore, Pakistan; 6Department of Pharmaceutics, Faculty of Pharmaceutical sciences, GC University, Faisalabad, Pakistan; 7Institute of Molecular Biology and Biotechnology, Bahauddin Zakariya University, Multan, Pakistan; 8Department of Pharmacology, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan; 9College of Pharmacy, University of Sargodha, Sargodha, Pakistan; 10Pharmacognosy Lab,Department of Botany, University of Chitral, Chitral, KPK, Pakistan; 11Akson College of Pharmacy, Mirpur University of Science & Technology (MUST), Mirpur, AJ&K, PakistanCorrespondence: Khizar Abbas, Department of Pharmacognosy, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan, Tel +923228832872, Email khizarabbas@bzu.edu.pkBackground: Nature represents a basic source of medicinal scaffolds that can develop into potent drugs used in the treatment of many diseases.Aim: The present study was planned to evaluate the combined effects of polyherbal methanolic extract of the herbs (fruit of capsicum, bark of cinnamon, rhizome of turmeric and rhizome of ginger) that were individually well known for their analgesic and anti-inflammatory activities. Furthermore, we aimed to develop hydrogel formulation of this polyherbal extract and to characterize and evaluate its analgesic and anti-inflammatory potential.Materials and Methods: Zingiber officinale (R.), Capsicum annuum (L.), Curcuma longa (L.), and Cinnamomum verum (J.) polyherbal extract (GCTC) was prepared by maceration and evaluated for analgesic and anti-inflammatory potential. Then, two different types of hydrogel formulation were prepared. One is pH-based hydrogel in which carbopol-940 was used and the other is temperature-based gel in which methocel-K100 was used as gelling agent. Different concentrations of polyherbal extract (GCTC), at 1%, 3% and 5%, were used in hydrogel formulation. These prepared hydrogel formulations were characterized and evaluated for analgesic and anti-inflammatory potential.Results: Results show that polyherbal extract and all the developed formulations of polyherbal extract (GCTC), at concentrations of 1%, 3% and 5%, have significant analgesic and anti-inflammatory effects with good appearance, homogeneity, spreadability, extrudability and stability.Conclusion: It was concluded from this project that polyherbal extract (GCTC) and its hydrogel have significant analgesic and anti-inflammatory potential.Graphical Abstract: Keywords: inflammation, formulation, carbopol, methocel, carrageenan

Nanogels combine the properties of hydrogels and nanocarrier systems, resulting in very effective drug delivery systems, including for cutaneous applications. Cyclodextrins (CDs) have been utilised to enhance the nanogels' loading ability towards poorly soluble drugs and promote/sustain drug release. However, formation of CD-based nanogels requires the use of specially modified CDs, or of crosslinking agents. The aim of this work was to develop a CD-based nanogel to improve the cutaneous delivery of ibuprofen by using the soluble β-cyclodextrin/epichlorohydrin polymer (EPIβCD) without adding any potentially toxic crosslinker. The use of EPIβCD enabled increasing ibuprofen loading due to its complexing/solubilizing power towards the poorly soluble drug and prolonging drug release over time due to the nanogel formation. DLS analysis proved that EPIβCD allowed the formation of nanostructures ranging from 60 up to 400 nm, depending on the gelling agent type and the gel preparation method. EPIβCD replacement with monomeric HPβCD did not lead in any case to nanogel formation. Permeation experiments using skin-simulating artificial membranes proved that the EPIβCD-based nanogel enhanced ibuprofen solubility and release, increasing its permeation rate up to 3.5 times, compared to a reference formulation without CD and to some commercial gel formulations, and also assured a sustained release. Moreover, EPIβCD replacement with HPβCD led to a marked increase in drug solubility and initial release rate, but did not provide a prolonged release due to the lack of a nano-matrix structure controlling drug diffusion. [ABSTRACT FROM AUTHOR]

Urticaria affects all age groups of a population. It is triggered by allergens in foods, insect bites, medications, and environmental conditions. Urticaria is characterized by itching, a burning sensation, wheals and flares, erythema, and localized edema. The aim of this study was to develop a polymeric dosage form of ebastine using Carbopol 940 and mixture of span and tween. The emulsion was prepared, the gelling agent was added and the desired emulgel loaded with active drug was formulated. The formulations were subjected to physical stability, pH, viscosity, spreadability, drug content analysis, thermal analysis, in vitro drug release, and in vivo anti-allergic activity in animal model. The formulated emulgel exhibited good physical stability. The pH of the formulation was in the range of 5.2 ± 0.17 to 5.5 ± 0.20 which is suitable for topical application. Insignificant changes (p>.05) were observed in viscosity and spreadability of stored emulgels. The drug content was in the official limit of Pharmacopeia (i.e. 100 ± 10%). DSC measurements predicted that there is no interaction between the active moiety and excipients in emulgel formulation. The optimized formulation (ES3) released 74.25 ± 1.8% of ebastine after 12 h. The ebastine emulgel showed significant (p<.05; ANOVA) in vivo anti-allergic activity as compared to commercial product BenadrylVR in histamine-induced allergy in rabbits. This study concluded that a topical drug delivery of ebastine-loaded emulgel could be well tolerated and safe for the treatment of urticaria/hives. [ABSTRACT FROM AUTHOR]

Current vaginal formulations, such as gels and pessaries, have limitations, including poor retention. Therefore, the use of mucoadhesive formulations that adhere to the vaginal wall would allow prolonged retention and controlled drug release while reducing the required dose and the potential toxicity associated with high drug loading. The aim of the current research was to develop, characterize, and optimize freeze-dried wafers loaded with metronidazole (MTz) to treat vaginal bacterial infections. Blank (BLK) composite wafers comprising carrageenan (CARR) and sodium alginate (SA) were initially formulated; however, due to poor physico-chemical properties, Carbopol (CARB), hydroxypropylmethylcellulose (HPMC), and polyethylene glycol 200 (PEG) were included. The MTz-loaded formulations were obtained by loading optimized composite CARB:CARR- or CARB:SA-based gels (modified with HPMC and/or PEG) with 0.75% of MTz prior to freeze-drying. The physico-chemical properties were investigated using texture analysis (resistance to compressive deformation and adhesion), scanning electron microscopy (SEM), X-ray diffractometry (XRD), and attenuated total reflectance Fourier-transform infrared (ATR-FTIR) spectroscopy. Functional properties were investigated by examining the swelling, porosity, drug release, and in vitro antimicrobial activity using E. coli as a model infection-causative agent. The results showed that HPMC and PEG generally improved the wafer's appearance, with smoother surfaces for easy insertion. From the physico-chemical characterization studies, only two composite wafers prepared from 8% CARB:SA 1:4 and 8% CARB:SA 1:9 gels were deemed optimal and loaded with MTz. Both formulations showed sustained drug release and achieved almost 100% cumulative release within 72 h in simulated vaginal fluid. The data obtained from the drug dissolution (release) experiments were fitted to various mathematical equations and showed the highest correlation coefficient with the Higuchi equation, suggesting a drug release based on diffusion from a swollen matrix; this was confirmed by the Korsmeyer–Peppas equation. The released MTz inhibited the growth of the E. coli used as a model bacterial organism. [ABSTRACT FROM AUTHOR]

The objective of the current study was to synthesize and characterize carbopol containing hydrogels with different monomers such as methacrylic acid (MAA), 2-acrylamido-2-methylpropane sulfonic acid (AMPS) and itaconic acid (ITA). Free radical polymerization method was optimized for the preparation of different formulations using N,N-methylene bis-acrylamide (MBA) as cross linking agent. Different studies were performed to evaluate the effect of different monomers on swelling, drug loading and drug release. Itopride Hydrochloride was used as model drug. FTIR, TGA, DSC and SEM were performed to probe the characteristics of fabricated hydrogels. Swelling studies of different fabricated hydrogels were performed in three pH conditions (1.2, 4.5 & 6.8). Higher swelling was observed at pH 6.8. An in-vitro release study was performed on pH 1.2 and 6.8. The synthesized hydrogels exhibited excellent mechanical strength, higher drug loading, pH sensitive and time dependent release up to 30 h. The excellent mechanical strength and extended drug release of Carbopol-co-poly-MAA-ITA hydrogels make them a potential candidate for controlled delivery of Itopride hydrochloride. [ABSTRACT FROM AUTHOR]

The development of semisolid formulations, gels in particular, has raised the attention of scientists more and more over the last decades. Because of their biocompatibility, hydrophilic nature, and capacity of absorbing large quantities of water, hydrogels are still one of the most promising pharmaceutical formulations in the pharmaceutical industry. The purpose of this study is to develop an optimal formulation capable of incorporating a water-poorly soluble active ingredient such as miconazole used in the treatment of fungal infections with Candida albicans and Candida parapsilosis. A D-optimal design was applied to study the relationship between the formulation parameter and the gel characteristics. The independent parameters used in this study were the Carbopol 940 concentration (the polymer used to obtain the gel matrix), the sodium hydroxide amount, and the presence/absence of miconazole. Ten different dependent parameters (Y1–Y10) were evaluated (penetrometry, spreadability, viscosity, and tangential tension at 1 and 11 levels of speed whilst destructuring and during the reorganization of the gel matrix). The consistency of the gels ranged from 23.2 mm (GO2) to 29.6 mm (GM5). The least spreadable gel was GO7 (1384 mm2), whilst the gel that presented the best spreadability was GO1 (3525 mm2). The viscosity and the tangential stress at the selected levels (1 and 11) varied due to the different compositions of the proposed gels. The gels were also tested for drug content and antifungal activity. All determinations had satisfying results; the drug content was within limits accepted by Ph. Eur. 10 and all formulations containing miconazole exhibited antifungal activity. An optimal formulation with miconazole was attained, consisting of 0.84% Carbopol 940 and 0.32% sodium hydroxide. [ABSTRACT FROM AUTHOR]

The aims of this study were to develop topical liposomal hydrogels based on thermal waters (TWs) acquired in the region of Biskra (Northeast Algeria) and also to investigate their rheological properties. Liposomes containing two highly mineralized thermal waters, Baraka (BTW) and Salhine (STW), were prepared by probe sonication using phosphatidylcholine (PC) and cholesterol (Chol), plain or mixed with phosphatidylglycerol (PG). Based on their lipid composition, obtained liposomes presented vesicle sizes of 60 nm, a low polydispersity index, and various negative zeta potentials. It was noted that with increasing counterions charge in TWs the zeta potential of liposomes decreased toward neutral values. Carbopol (1%, w/w) hydrogels prepared with BTW, STW, and also demineralized water (placebo hydrogel) showed a non-Newtonian behavior, pseudoplastic fluid adjusted to Carreau model. The composition of thermal waters influenced highly the rheological properties of Carbopol hydrogels. Liposomal hydrogels were prepared by dispersing liposomes in hydrogels formulated with the same encapsulated thermal water. Regardless of composition or lipid concentration of added liposomes, the viscosity and viscoelastic parameters of Carbopol hydrogels changed negligibly. Indeed, liposome composition and lipid concentration seemed to have no effect on the rheological properties of Carbopol hydrogel in the presence of an important charge of cations. Hence, hydrogels and liposomal hydrogels based on thermal waters had suitable rheological properties for topical application and delivery of minerals in the skin. [ABSTRACT FROM AUTHOR]