Dhiman Sonia, Mannan Ashi, Mohan Maneesh, Singh Thakur Gurjeet
Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Curr Drug Res Rev. 2025 Aug 25. doi: 10.2174/0125899775386780250813111412.
The oral route is a preferred method for drug administration; however, lipophilic drugs often suffer from poor water solubility, significantly limiting their therapeutic effectiveness. Traditional approaches like complexation, micronization, and solid dispersion have been explored, but each comes with inherent limitations.
Self-Emulsifying Drug Delivery Systems (SEDDS) have emerged as a promising strategy to address solubility challenges. These systems incorporate drug molecules into a mixture of oils, surfactants, and cosolvents to enhance solubility. Ternary phase diagrams are frequently utilized to determine optimal component ratios for effective formulation.
SEDDS maintain drugs in a solubilized form within gastrointestinal fluids and protect peptide drugs from enzymatic degradation-a common issue in conventional formulations. They also facilitate the formation of stable emulsions at the target site, enhancing drug absorption. Additionally, the ability of SEDDS to traverse the blood-brain barrier (BBB) increases their applicability in treating neurological disorders.
The findings emphasize the utility of SEDDS in overcoming the solubility and stability challenges faced by poorly water-soluble drugs. Their capacity to enhance drug absorption and protect bioactive molecules from degradation aligns with current efforts to improve oral drug delivery systems. However, formulation complexities and variability in in vivo performance remain areas requiring further investigation.
This review outlines the formulation strategies, characterization methods, and evaluation techniques for SEDDS, emphasizing their potential in enhancing the bioavailability of poorly soluble drugs, particularly those aimed at the central nervous system. SEDDS offer a promising platform for improving therapeutic outcomes across diverse clinical settings.
口服途径是药物给药的首选方法;然而,亲脂性药物通常水溶性较差,这显著限制了它们的治疗效果。人们已经探索了诸如络合、微粉化和固体分散等传统方法,但每种方法都有其固有的局限性。
自乳化药物递送系统(SEDDS)已成为解决溶解性挑战的一种有前景的策略。这些系统将药物分子纳入油、表面活性剂和助溶剂的混合物中以提高溶解度。三元相图经常被用于确定有效制剂的最佳组分比例。
SEDDS能使药物在胃肠液中保持溶解状态,并保护肽类药物不被酶降解——这是传统制剂中常见的问题。它们还能促进在靶部位形成稳定的乳剂,增强药物吸收。此外,SEDDS穿越血脑屏障(BBB)的能力增加了它们在治疗神经疾病方面的适用性。
这些发现强调了SEDDS在克服水溶性差的药物所面临的溶解性和稳定性挑战方面的实用性。它们增强药物吸收和保护生物活性分子不被降解的能力与当前改善口服药物递送系统的努力相一致。然而,制剂复杂性和体内性能的变异性仍是需要进一步研究的领域。
本综述概述了SEDDS的制剂策略、表征方法和评估技术,强调了它们在提高难溶性药物生物利用度方面的潜力,特别是那些针对中枢神经系统的药物。SEDDS为改善不同临床环境下的治疗效果提供了一个有前景的平台。