The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.
Naproxen is a nonsteroidal anti-inflammatory drug, it has analgesic, anti-inflammatory and antipyretic effect by inhibiting prostaglandin synthesis via inhibition of cyclooxygenase enzymes. This study was designed to evaluate analgesic and Anti-inflammatory effect of optimized NANEs (Non-aqueous Nano Emulsion) of Naproxen in experimental animals. The anti‐inflammatory activity of the optimized NANEs of Naproxen was evaluated using right hind paw oedema size of rats induced by carrageenan injection and analgesic effect was evaluated using Hot Plate method and Tail-flick method applied on rats. Results related to the anti‐inflammatory activity revealed that the optimized NANEs of Naproxen produced a maximum percent oedema inhibition as compared to standard naproxen formulation. Similarly, the analgesic effect of the optimized NANEs of Naproxen shows better effect as compared to marketed formulations. Finally, this study concludes that the tested Optimized NANEs of Naproxen exhibited good and acceptable anti-inflammatory and analgesic effect in comparison to the commercial marketed formulation.
Microsponge, a novel drug delivery system, is designed to deliver a pharmaceutically active ingredient efficiently at the minimum dose. Microsponge plays an important role in enhancing drug stability, reducing side effects, and modifying drug release profiles. It is mostly used for transdermal delivery. Recent studies also explored their use for oral administration. This study aimed to explore the potential use of the microsponge technique in improving the aqueous solubility and dissolution profile of pentoxifylline (PTX). In this study, microsponges were prepared by a quasi-emulsion solvent diffusion method by varying concentrations of carriers. Nine different ratios of the PTX:Eudragit E-100 with varying amounts of dichloromethane were used. All formulated microsponges were evaluated for %production yield, compatibility of drug excipient, encapsulation efficiency, in vitro drug release, and in vivo bioavailability, as well as recorded by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). Our data suggested that the aqueous solubility of PTX microsponges was four times greater than that of pure drug. The in vitro drug release of selected microsponges (M8) was found to be 70%; furthermore, the in vivo study suggested that the selected formulation significantly enhanced drug concentration in the plasma (9,219 ng/mL in 12 hours) in comparison to pure drug PTX (2,476 ng/mL in 12 hours). SEM showed that the prepared microsponges were spherical with porous nature. Fourier-transform infrared spectroscopy and DSC studies confirmed an absence of incompatibility among drugs and selected excipients. The pH of the selected gel was found to be 6.8, which was compatible with those of skin and oral formulations also. All above data suggested a highly successful and beneficial use of the microsponge technique in enhancing aqueous solubility, dissolution profile, and oral bioavailability of PTX. Microsponge-based delivery of PTX may represent an alternative strategy to improve the bioavailability of the drug.
Aim: The enhancement of oral bioavailability of sertraline (SRT) hydrochloride (HCl) using the nanoprecipitation and solvent diffusion techniques for stable nanosuspension. Materials and Methods: There have been still few of published researches on the formulation of SRT HCl using solid dispersion, fast dissolving tablet, and selfmicroemulsifying drug delivery systems. Nanosuspension was prepared separately by using different techniques and different polymers (Eudragit RL 100 and PVP K 25). The in vitro dissolution study was performed as per the USP paddle method in 0.1N HCl. The crystalline structure of the drug, the molecular interaction, morphology, and particle size of nanosuspension were also investigated. Results and Discussion: The nanoprecipitation method with drug and PVP K 25 (1:1) showed its potential in the enhancement of the drug release rate (99% in 45 min). The synergistic effects of reduction of drug crystallinity and particle size could increase the dissolution rate of SRT HCl by providing a stable nanosuspension. The in vivo study demonstrated that the maximum plasma concentration and area under the curve values of selected nanosuspension in rabbits were found greater than that of the commercial tablets (tablet potiga, 50 mg) and standard SRT HCl. Conclusion: This work may contribute to a new strategy for enhancement oral bioavailability of SRT HCl.
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