This study aims to formulate azithromycin oleogel to locally treat skin infections such as acne vulgaris and skin wound infection. Providing a form of azithromycin that can be administered topically is highly desired to prevent unwanted systemic complications including diarrhea, nausea, and abdominal pain. Additionally, it will avoid first pass metabolism, improves patient acceptance, provides an alternative in nauseated patients, decreases the dose by direct contact with the pathological site, and provides a noninvasive and convenient mode of administration. Furthermore, for treating wound infections, the gel will act as a scaffold biomaterial for wound closure besides its antibacterial effect. Herein, we propose the use of grapeseed oil-based oleogel with glycerol monostearate (GMS) as an organogelator as a promising strategy for the effective topical delivery of azithromycin. A series of oleogels were prepared by varying concentrations of organogelators namely GMS, palmitic acid, Compritol 888, and stearic acid, while maintaining the weight ratio of grapeseed oil and clove oil constant. Initial evaluation showed azithromycin oleogel with 15% GMS to be the optimum formulation and it was selected for further evaluation. In vivo testing of the formulated gel showed significant effectiveness in promoting faster clinical healing of Staphylococcus aureus infected wounds. The findings of the present study suggest that azithromycin oleogel is stable, safe, cost-effective, and it provides significant antibacterial activity. © 2022, The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.
Selexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MoreIsradipine belong to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is used in the treatment of hypertension, angina pectoris, in addition to Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, therefore, oral bio-availability will be approximately15 to 24 %.
The aim of this study was to formulate and optimize a stable nanoparticles of a highly hydrophobic drug, isradipine by anti-solvent microprecipitation Method to achieve the higher in vitro dissolution rate, so that it will be absorbed by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism&nbs
... Show MoreThe objective of the study was to develop microneedle (MN) patch, with suitable properties to ensure the delivery of a therapeutic level of lornoxicam (LXM) in a period suitable to replace parenteral administration in patients, especially those who fear needles. The used polymers were cold water-soluble polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP) of low molecular weight with PEG 400 as plasticizer and Tween 80 (to enhance the release) using micro molding technique. Patches were studied for needle morphology, drug content, axial fracture force measurement and drug release while the optimized formulas were further subjected to pH measurement, folding endurance, ex vivo permeation study, histopathology study, stability study and
... Show MoreAlpha-tocopherol acetate is one of the most important vitamin E derivatives,that were used as antioxidants. Adsorbents like kaolin, magnesium carbonate, and microcrystalline cellulose were used successfully to incorporate oily alpha-tocopherol acetate into an acceptable powder dosage form. The results revealed that microcrystalline cellulose as an adsorbents gave the best results with 50% loading capacity at time, 8 minutes before and after incubation period (3 months at 30C°), while kaolin and magnesium carbonate have been shown a significant difference before and after incubation. Addition of 1% w/w magnesium carbonate to the kaolin enhanced the loading capacity by decreasing the time of adsorption from 20 to 6 minutes and 47
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The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibi
... Show MoreFlurbiprofen (FLB) is chemically 2-(3- fluoro-4-phenyl phenyl) propanoic acid. It is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis and osteoarthritis. Oral administration of this drug is associated with severe gastrointestinal side effects like ulceration and gastrointestinal bleeding. The solution to this problem lies in the fact that topically applied NSAIDs are safer than orally. This study aims to prepare different topical semisolid formulation of FLB as cream base (o/w), (w/o) and gel base using different gel-forming agents in different concentrations. Comparing characterization properties in addition to release and diffusion study for all the prepared formulas to select the best on
... Show MoreClotrimazole nail lacquer was created using this research, which also included the incorporation of two different kinds of polymers. (Eudragit RL 100 and ethyl cellulose) in various concentrations, as well as castor oil as a plasticizer, salicylic acid as a keratolytic agent, and N-acetylcysteine as a penetration enhancer. The objective was to optimize the selection of polymers and their concentrations to enhance release efficacy based on in vitro permeability experiments, while also ensuring favorable film characteristics, such as flexibility, gloss, adhesive qualities, drying time, non-volatile content, viscosity, and water resistance. Formulation F3 was selected as the superior formula considering several parameters, including excellent
... Show MoreMeloxicam is a non-steroidal anti-inflammatory drug. It is practically insoluble in water. It is associated with gastrointestinal side effects at high doses on long term treatment. The aim of this investigation to formulate and evaluate gellified nanoemulsion of meloxicam as a topical dosage form to enhance meloxicam therapeutic activity and reduce systemic side effect.
The pseudo ternary phase diagrams were made, including the oil mixture which is composed of almond oil and peppermint oil at a ratio (1:2), variable surfactant mixture (S mix) which are tween 80 and ethanol at ratios of (1:1, 2:1, 3:1, and 4:1) and double distilled water. Slow dripping of double distilled water to the combination of the oil mixtu
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