The main aim of the study was to develop and statistically optimize the proniosomal gel for enhanced transdermal delivery using 32 factorial designs to investigate the influence of both non-ionic surfactant and cholesterol to maximize the entrapment efficiency and flux. The concentration of non-ionic surfactant and cholesterol were taken as independent variables, while entrapment efficiency and flux were taken as dependent variables. The study showed that the entrapment efficiency depends on both cholesterol and surfactant, whereas permeation flux depends only on the surfactant. Proniosomal gel showed a significantly enhanced drug permeation through the skin, with an enhancement ratio 3.81±1.85 when compared to the drug solution. Comparative evaluation of permeation studies and the in vitro release study of optimized proniosomal gel (F5) with that of marketed gel and carbopol gel showed that the penetration of the optimized formulation was enhanced 1.75 times in comparison with that of the marketed formulation, and the release was in a controlled manner. Similarly, the anticandidial activity showed a significantly higher activity (p<0.05) than the marketed and carbopol gel. This may be due to the enhanced penetration of noisome-containing drug through the fungal cell wall, inhibiting the ergo sterol synthesis, thereby causing the fungal cell death due to the presence of penetration enhancer. The stability study at two different temperatures (30 ± 2°C and 4 ± 2°C) confirmed that the formulations were stable even at the end of 45 days. Hence, proniosomal gel is an efficient carrier for the delivery of clotrimazole, thereby prolonging the action.
The challenge faced by the majority of the pharmaceutical products is the poor solubility of the drug candidates which leads to low bioavailability. Liquisolid compact is one of the emerging techniques that enhances the dissolution of poorly water soluble drugs. Liquisolid system mentions to the formulation made by the transforming the liquid drug, either in the form of suspension or solution in non volatile solvents into a dry, non-sticky, free-flowing and compactable powder mixtures. This is achieved by mixing the suspension or solution of the drug with appropriate carriers and coating agents. The technology has the ability to increase aqueous solubility, rate of dissolution and absorption of poorly soluble drug by keeping it in molecularly dispersed form leading to its improved bioavailability when compared to conventional tablets. Liquisolid technology is the impending approach for enhancing the solubility of poorly water-soluble drug by adopting simple manufacturing process and low production cost.
Background:The gastro-retentive system is one of the promising oral drug delivery system due to its ability to remain in the gastric region for a longer period. This helps in improving the bioavailability by increasing the solubility and reducing drug wastage. Approach: Various approaches have been put forward to achieve the gastro-retentive property. Among them, floating (hollow) microsphere is the most prominent approach. Findings: Hollow microspheres are spherical free flowing powders in the size range of 1-1000 m without core. It is prepared using proteins or synthetic polymers. This buoyant system improves gastric retention, sustains the drug release, and hence reduces the fluctuations in plasma drug concentration. Conclusion: This review presents an insight into recent advances in methods of fabrication, evaluation and applications of hollow microspheres as gastro-retentive drug delivery systems.
According to WHO, dental caries is the most prevalent oral disease, and its progression leads to tooth loss. Clinical management of caries focuses on the severity and extent of disease with the main aim, i.e., the 'art' of creating a good restoration. Recently, it has been reported that aspirin can stimulate existing stem cells and regenerate damaged teeth. But, the therapeutic effectiveness of a drug depends on developing a suitable novel drug delivery system, to retain at the site and suitably release the drug to produce effective therapy. Therefore, the present investigation intends to develop Aspirin-Poly lactic-co-glycolic acid microspheres for the restoration of dentin. Materials and Methods: Aspirin-Poly lactic-co-glycolic acid microsphere was formulated by the double emulsion technique and evaluated for particle size, encapsulation efficiency, characterization (differential scanning calorimetry, X-ray powder diffraction), in vitro release, as well as irritation testing using the Hen's egg test-chorioallantoic membrane method. Results: The formulation exhibited good encapsulation efficiency (87.31±1.52%) and a particle size of 7.52 μm by Scaning Electron Micrscopy. In vitro release study exhibited sustained release (98.76±0.49%) for 16 days and triphasic release. This confirms that release is due to polymer erosion, swelling, and degradation. The ex vivo permeation study also confirmed sustained permeation and showed the significant partition and accumulation of the drug in the tissue. Further, the prepared formulation showed significantly low irritation compared to positive control by Hen's Egg Test-Chorioallantoic Membrane method. Conclusion: Thus, the above finding suggests that the formulation can stimulate stem cells for the regeneration of dental tissue.
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