脂质体增强口服药物吸收的潜力。,Current Drug Delivery

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脂质体增强口服药物吸收的潜力。
Current Drug Delivery ( IF 2.8 ) Pub Date : 2016-01-16 , DOI: 10.2174/1567201813666160115125756
Marjan Daeihamed , Simin Dadashzadeh ₁ , Azadeh Haeri , Masoud Faghih Akhlaghi

Affiliation

考虑患者依从性时，口服药物是第一选择。但是，许多障碍面临着药物的口服吸收，从而限制了约90％的治疗药物的生物利用度。利用纳米颗粒药物递送系统是增加口服吸收的主要策略。它们可以通过诸如保护胃肠道中的药物，增加药物在细胞中的细胞接触和停留时间，保护药物免受系统内新陈代谢和外排以及增加跨粘膜和上皮层的扩散等机制来改善口服生物利用度。脂质体是生物相容性载体，用于改善药物的口服生物利用度，除了纳米载体用于口服给药的一般优势外，它们还具有脂质双层结构的优点。它们可以更好地粘附于生物膜，与胆盐形成混合胶束结构，以增加难溶性药物的溶解度，并且适合淋巴吸收。他们已经成功地改善了包括肽和蛋白质，亲水性和亲脂性药物在内的多种化合物的口服生物利用度。在胃肠道条件下的稳定性是口服脂质体的主要关注点，但是，已经提出了有希望的方法来增加口服脂质体的稳定性。这些措施包括：使用适当的脂质组合物，聚合物涂层，在脂质体结构中添加稳定脂质，制备双重脂质体和脂质体原以及其他一些创新方法。本综述着眼于脂质体在改善药物口服吸收中的作用，所遇到的问题，以及旨在克服这些问题的脂质体类型。将讨论口服传递的障碍，并研究封装在各种类型脂质体中时生物利用度提高的实例。

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Potential of Liposomes for Enhancement of Oral Drug Absorption.

Oral administration of medication is the first option when patient compliance is considered. However, many barriers face oral absorption of drugs that limit bioavailability in about 90% of therapeutic agents. Utilization of nanoparticulate drug delivery systems is a major strategy for increasing oral absorption. They can improve oral bioavailability through mechanisms such as protection of the drug in the GI tract, increasing cellular contact and residence time of the drug, protection of the drug from presystemic metabolism and efflux and increasing diffusion across the mucosal and epithelial layers. Liposomes are biocompatible carriers employed to improve oral bioavailability of drugs and in addition to the general advantages of nanocarriers for oral delivery, they offer benefits derived from their lipidic bilayer structure. They can better adhere to biomembranes, form mixed-micelle structures with bile salts to increase the solubility of poorly-soluble drugs and are suitable candidates for lymphatic uptake. They have been successful in improving oral bioavailability of a variety of compounds including peptide and proteins, hydrophilic and lipophilic drugs. Stability under GI conditions is the main concern for oral liposomes, however, promising approaches have been suggested to increase the stability of oral liposomes. These include: using appropriate lipid compositions, polymer coating, addition of stabilizing lipids to liposomal structures, preparation of double liposomes and proliposomes and some other innovative methods. The present review focuses on the role of liposomes in improving oral absorption of drugs, the problems encountered, and the types of liposomes designed to overcome these issues. Barriers to oral delivery will be discussed and examples of bioavailability enhancement upon encapsulation in various types of liposomes investigated.

更新日期：2019-11-01

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