Rajabalaya Rajan, Musa Muhammad Nuh, Kifli Nurolaini, David Sheba R
PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Brunei Darussalam.
Drug Des Devel Ther. 2017 Feb 13;11:393-406. doi: 10.2147/DDDT.S103505. eCollection 2017.
Liquid crystal (LC) dosage forms, particularly those using lipid-based lyotropic LCs (LLCs), have generated considerable interest as potential drug delivery systems. LCs have the physical properties of liquids but retain some of the structural characteristics of crystalline solids. They are compatible with hydrophobic and hydrophilic compounds of many different classes and can protect even biologicals and nucleic acids from degradation. This review, focused on research conducted over the past 5 years, discusses the structural evaluation of LCs and their effects in drug formulations. The structural classification of LLCs into lamellar, hexagonal and micellar cubic phases is described. The structures of these phases are influenced by the addition of surfactants, which include a variety of nontoxic, biodegradable lipids; these also enhance drug solubility. LLC structure influences drug localization, particle size and viscosity, which, in turn, determine drug delivery properties. Through several specific examples, we describe the applications of LLCs in oral and topical drug formulations, the latter including transdermal and ocular delivery. In oral LLC formulations, micelle compositions and the resulting LLC structures can determine drug solubilization and stability as well as intestinal transport and absorption. Similarly, in topical LLC formulations, composition can influence whether the drug is retained in the skin or delivered transdermally. Owing to their enhancement of drug stability and promotion of controlled drug delivery, LLCs are becoming increasingly popular in pharmaceutical formulations.
液晶(LC)剂型,尤其是那些使用基于脂质的溶致液晶(LLC)的剂型,作为潜在的药物递送系统已引起了广泛关注。液晶具有液体的物理性质,但保留了一些结晶固体的结构特征。它们与许多不同类别的疏水和亲水化合物兼容,甚至可以保护生物制品和核酸不被降解。本综述聚焦于过去5年进行的研究,讨论了液晶的结构评估及其在药物制剂中的作用。描述了将溶致液晶分为层状、六方和胶束立方相的结构分类。这些相的结构受表面活性剂添加的影响,表面活性剂包括多种无毒、可生物降解的脂质;这些还能提高药物溶解度。溶致液晶结构影响药物定位、粒径和粘度,进而决定药物递送性能。通过几个具体例子,我们描述了溶致液晶在口服和局部药物制剂中的应用,后者包括透皮和眼部给药。在口服溶致液晶制剂中,胶束组成和由此产生的溶致液晶结构可以决定药物的溶解和稳定性以及肠道转运和吸收。同样,在局部溶致液晶制剂中,组成可以影响药物是保留在皮肤中还是通过透皮递送。由于溶致液晶增强了药物稳定性并促进了药物的控释,它们在药物制剂中越来越受欢迎。