Abstract

Objective: The objective of this work was to improve the solubility and dissolution rate of Nifedipine by preparing a solid-self micro emulsifying drug delivery system (Solid-smedds).
 Methods: Liquid-self-emulsifying drug delivery system formulations were prepared by using linseed oil as oil, tween 80 as a surfactant and PEG 400 as cosurfactant. Components were selected by solubility screening studies and the self-emulsifying region was identified by the pseudo-ternary phase diagram. Thermodynamic stability study was performed for the determination of stable liquid-smedds formulation. These formulations were evaluated for self-emulsification time, drug content analysis, robustness to dilution test, particle size analysis, in vitro diffusion study, and Stability study. Solid self-micro emulsifying formulations were prepared by using aerosil-200 at a different ratio. Lf9S (0.65:1) was selected due to its highest drug entrapment efficiency and a decrease in particle size. It was selected for further studies into DSC, SEM, FTIR, and XRD analysis.
 Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM study, it was observed that the drug has been uniformly distributed and having a smooth surface. From the in vitro dissolution study, it improved the dissolution rate of nifedipine which was 98.70% of drug release where pure drug release only 6.72%.
 Conclusion: In conclusion, a solid self-micro emulsifying drug delivery system is improved the solubility and drug release rate but also improved the stability of the formulation.

Highlights

  • Around 40% of recent drug candidates become poor water solubility and the oral deliveries of those medicines are usually related to high intrasubject and inter-subject variability, a lack of dose proportionality, low bioavailability

  • For the analysis of solubility with nifedipine linseed oil, soybean oil, and almond oil were as oil, tween 60, tween 40, span 20 and tween 80 were as a surfactant and PEG 400, PEG 200, PPG, PEG 600 were taken as cosurfactants

  • Solid-self emulsifying drug delivery system of nifedipine was successfully prepared by using linseed oil as oil part, Tween 80 as a surfactant, PEG 400 as co-surfactant and Aerosil 200 as adsorbent

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Summary

Introduction

Around 40% of recent drug candidates become poor water solubility and the oral deliveries of those medicines are usually related to high intrasubject and inter-subject variability, a lack of dose proportionality, low bioavailability To overcome these issues, several formulation ways are utilized together with specific utilization of surfactants, lipids, permeation enhancers, micronization, salt formation, cyclodextrins, solid dispersion. SEDDS or self-emulsifying oil formulations (Seof) outlined as isotropic mixtures of natural or synthetic oils, solid or liquid surfactants or instead, one or additional hydrophilic solvents and co-solvents/surfactants [1]. On delicate agitation, these systems will form fine o/w emulsions (oil-in-water) or self-micro emulsifying drug delivery system (SMEDDS) or microemulsions followed with dilution into liquid media, like epithelial duct (GI) fluids [2]. SEDDS effectively produce emulsions with a droplet size range of 100-200 nm for SMEDDS whereas SNEDDS produce less than 100 nm [3]

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