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Acitretin is the drug of choice for the treatment of psoriasis, but due to its poor solubility, the development of oral and topical formulations of acitretin has been restricted. The aim of the present investigation was to enhance the solubility of acitretin. Solid dispersions of acitretin were prepared using a lipidic solubilizer, Gelucire® 44/14. These solid dispersions were characterized through FT-IR, DSC, XRD, drug content and solubility studies. The most solubilized dispersion was loaded on an N,N-methylenebisacrylamide microporous cryogel. Physical parameters of the solubilized drug such as the porosity, rheological behaviour, surface properties, appearance, drug content and diffusion behaviour were studied. It was concluded that the solubilized form of acitretin, loaded on a surface-modified cryogel, is the best option for the treatment of psoriasis. The hydration of the skin was excellent, and the permeability of the acitretin into the skin was better. [ABSTRACT FROM AUTHOR]

Oral conventional formulations like tablets, capsules and liquids have many limitations. Due to this and patient incompliance, there is a need to develop new formulations with better efficiency and stability. The aim of the present study was to develop and optimize fast dissolving Oro-dispersible strips (ODS) of isosorbide mononitrate by 3²-full factorial design. HpMC E15 (X1) concentration and glycerin (X2) concentration were selected as the independent variables, whereas, in vitro disintegration time (Y1), percent drug release (Y2) and tensile strength (Y3) were selected as dependent variables. Fast dissolving Oro-dispersible strips of isosorbide mononitrate were prepared by the solvent casting method.Tensile strength, disintegration time and in vitro dissolution of ODS of the strip were found to be within accepted range for optimized formulation. Statistical validity of the polynomials was established by ANOVA using Design-Expert software. The study suggests isosorbide mononitrate fast dissolving Oro-dispersible strip as potential alternative dosage form in management of angina pectoris. [ABSTRACT FROM AUTHOR]

Success of any healthcare product is based on its performance, which is further dependent upon the quality of the product. Quality of the polyherbal ayurvedic formulation is assured by developing proper analytical standards with the help of the guidelines provided by CCRAS (Central Council for Research in Ayurvedic Sciences), which will also ensure its authentication. Ayush-64 is a polyherbal formulation and its analytical standards were developed for various parameters like organoleptic properties, physicalchemical and chromatographic profiling etc. These standards were developed by studying and analyzing three batches of self-manufactured Ayush-64 tablets with the help of good manufacturing practices (GMP). These parameters were found to be sufficient to standardize and authenticate the quality of the formulation, which can be used further as a reference standard for quality control and quality assurance of the final product. [ABSTRACT FROM AUTHOR]

Drug release properties for transdermal route can be better modified as per requirement which is mostly dependent upon the carrier system. In case of organic film-forming systems, the physical properties may not be achieved for successful delivery of drug through transdermal route. A novel organic-inorganic hybrid film-forming gel may fulfil these expectations to many extend. The present study focuses on the development of the organic-inorganic hybrid film-forming gel. A smooth, transparent, clear film-forming gel of tramadol was prepared for application on the intact skin with better comfort and modified drug release rate properties. The key properties of the adhesive films produced from the hybrid gels were investigated and the results showed that the incorporation of appropriate PVA: TEOS: Glycerine: HCl in the ratio of 46:12.5:25.5:6 respectively. Resultant hybrid film-forming gel has modified the physical properties and improved drug release properties. Furthermore, the investigations of skin irritation suggested no irritation to skin after topical application. This study has provided an alternative to the presently available organic gel and films for transdermal delivery of drugs with better patient compliance and modified physical and chemical stability. [ABSTRACT FROM AUTHOR]

Targeted delivery of drugs at appropriate concentrations to ocular tissues is required to avoid wastage. Hence, advanced systems that maximize the release of poorly soluble drugs and deliver them at ocular sites must be designed. In this study, Soluplus® (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol–graft copolymer) was selected as a solubilizer as well as film former for preparing ocular inserts and polyethylene glycol 400 (PEG-400) as a plasticizer. On the basis of an initial phase solubility study, the maximum concentration of Soluplus® possible was used for developing the inserts. An optimized formulation was obtained using a 32-factorial design. Two factors at three levels were used to design the ocular inserts. Soluplus® (X1) and the plasticizer, PEG-400 (X2), were set as the independent variables at various levels, and the Rel4h (drug release in 4 h, Y1) and tensile strength (Y2) were set as the dependent variables. A pre-formulation study was conducted to select suitable materials. Various physico-chemical parameters of the optimized formulation, including the tensile strength and folding endurance, were studied using FT-IR, DSC, XRD, and SEM. An in vitro dissolution study was conducted to determine the amount of drug released. There was no redness, swelling, or watering of the rabbit eye. It was concluded that the ocular inserts of the poorly soluble nepafenac developed using a graft-co-polymer enhanced the solubility and utilization of the drug for a prolonged period. [ABSTRACT FROM AUTHOR]

Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). But the solubility and bioavailability of this drug are poor, which has restricted the design and development of dosage forms for efficient and successful therapy. The present study was carried out to develop nanocomposites using an amphiphilic graft co-polymer (Soluplus®) as a carrier to enhance the solubility and bioavailability of bosentan. The graft co-polymer-based nanocomposite formulation was prepared using the single-emulsion technique. The nanocomposite was characterised in terms of particle size analysis, solubility, percentage entrapment efficiency, drug-loading capacity, surface morphology, drug content, in vitro dissolution, stability and bioavailability. FT-IR study revealed that there was no interaction between the drug and Soluplus®. DSC analysis of the nanocomposite formulation confirmed that the bosentan was completely encapsulated within a Soluplus®. XRD analysis showed that the drug was converted to an amorphous form irreversibly. SEM images showed that the particles were of size 96–129 μm and had slightly smooth to rough textured surface. TEM analysis indicated that the diameters of the prepared bosentan nanocomposite after dispersion in distilled water were 13.69–96.78 nm. Statistically significant increases in the solubility, dissolution and bioavailability of the drug were observed. It was confirmed that the use of a graft co-polymer carrier-based nanocomposite formulation is a good approach for efficient delivery of bosentan, the solubility and bioavailability being increased manifold. [ABSTRACT FROM AUTHOR]

The aim of present study to enhance the solubility of quercetin, a poorly water soluble drug, quercetin containing blends (keeping total concentration 40% w/v, constant) was fabricated by mixed-solvency approach. In this technique, blends of solubilizers (sodium acetate, sodium citrate, urea as hydrotropic agent, propylene glycol, glycerin, PEG 200, PEG 400, PEG 600 as co solvents, PEG 4000, PEG 6000 as water soluble solvents etc.) have been employed to increase the solubility. The significant enhancement in solubility of drug in mixed solvents was observed in A4 blends which contain 10% sodium citrate, 5% sodium acetate and 25% S co-solvents (25% S co-solvents contains PG, glycerin, PEG 200, PEG 400, PEG 600, PEG 4000, PEG 6000). After improvement of solubility of quercetin in selected blends that incorporated into topical dosage form (prepared gel) by utilizing Carbopol ETD 2020 as gelling agent. The prepared blends and gel were evaluated for pH, surface tension, specific gravity and viscosity and in--vitro diffusion study, skin irritation studies, spreadability respectively. The characterization of pure quercetin, blend, and gel was performed by differential scanning calorimetry (DSC); X-ray diffraction (XRD) etc. From experimental work it was found that the prepared formulation is safe, effective, non-irritant, non-toxic and stable with good spreadability. The results showed that mixed solvency has valuable and unique strategy to ameliorating the solubility of lipophilic herbal anticancer component, quercetin. [ABSTRACT FROM AUTHOR]