聚乙二醇400助表面活性剂对BCSⅱ类模型药物微乳的影响

S. Taher, K. Al-kinani, Zahraa Mohsen Hammoudi, M. M. Ghareeb
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引用次数: 7

摘要

微乳是递送难溶性药物、保护不稳定药物、控制药物释放和提高药物生物利用度的一种有趣的方法。它们可以外用、口服或静脉注射,并使用聚乙二醇(PEG-400)作为助表面活性剂来改善生物分类系统(BCS) II类药物的溶解度和稳定性。本研究的目的是开发和测试一种水包油(O/W)微乳基配方,通过使用天然油和PEG 400作为助表面活性剂来改善疏水药物(卡维地洛)的溶解度和稳定性。采用水滴定法制备了水包油微乳液。通过pH、粒径、zeta电位和热力学稳定性研究对其进行优化,并进行体外释放实验。根据组分溶解度研究和伪三元相图,选择1:1比例的Tween80与PEG400 (Smix)制备最终微乳液。优选的ME4配方含有10%的油、42%的Smix和48%的水。平均粒径为58 nm, pH为6.95,zeta电位为28mV,透过率为97.1%。热力学稳定性研究数据表明,最终配方的稳定性较好。制备的ME制剂增强了药物的增溶效果,从而证实了ME系统作为更好地递送(BCS) II类的载体的实用性。
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Co-surfactant effect of polyethylene glycol 400 on microemulsion using BCS class II model drug
Microemulsions are an intriguing method for delivering poorly soluble drugs, protecting labile drugs, controlling drug release, and increasing drug bioavailability. They can be given topically, orally, or intravenously, and use polyethylene glycol (PEG-400) as a cosurfactant to improve the solubility and stability of biological classification system (BCS) class II drugs. The goal of this research is to develop and test an oil-in-water (O/W) microemulsion-based formulation to improve the solubility and possibly the stability of a hydrophobic medication (carvedilol) by using natural oil and PEG 400 as a co-surfactant. oil in water microemulsion was formulated using the water titration method. pH, particle size, zeta potential, and thermodynamic stability studies were carried out for optimization, followed by in vitro release experiments. Based on component solubility studies and pseudo-ternary phase diagrams, a 1:1 ratio of Tween80 to PEG400 (Smix) was chosen for the final microemulsion preparation. The optimized ME4 formula selected contains 10% oil, 42% Smix, and 48% water. The average globule size was found to be 58 nm, the pH was 6.95, the zeta potential was 28mV, and the percent transmittance was 97.1 percent. The thermodynamic stability study data shows better stability of the final formulation. The solubilization effect of the drug was enhanced by prepared ME formulation and hence confirms the utility of the ME system as a vehicle for better delivery of (BCS) class II.
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来源期刊
CiteScore
1.00
自引率
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发文量
30
期刊介绍: Journal of Advanced Pharmacy Education & Research [JAPER] aims to explore the knowledge of pharmacy professionals and cater the need of research and development activities of both academia and Industries. Further, also aimed to bridge the gap between theoretical aspects of drug delivery concepts and practical clinical studies to make sure of the novel drug delivery system usefulness in health care system. The Journal having scope for researchers engaged in drug delivery field to utilize the scientific contents in a rightful way. Journal of Advanced Pharmacy Education & Research [JAPER], a broad-based journal was founded on two key tenets: To publish the most exciting researches with respect to the subjects of Pharmaceutical science. Secondly, to provide a rapid turn-around time possible for reviewing and publishing, and to disseminate the articles freely for research, teaching and reference purposes. Our objective is to inform authors of the decision on their manuscript as early as possible. Following acceptance, a paper will normally be published in the next available issue. Journal of Advanced Pharmacy Education & Research [JAPER], is using online manuscript submission, review and tracking system for quality and quick review processing. Review processing is performed by the editorial board members of JAPER, outside experts; at least two independent reviewers approval followed by editor approval is required for acceptance of any citable manuscript.
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