Semalty Ajay
H.N.B. Garhwal University Srinagar (Garhwal), Department of Pharmaceutical Sciences, Chauras Campus , Chauras, Srinagar (Garhwal), 246174 , India
Expert Opin Drug Deliv. 2014 Aug;11(8):1255-72. doi: 10.1517/17425247.2014.916271. Epub 2014 Jun 7.
Poor solubility and dissolution of drugs are the major challenges in drug formulation and delivery. In order to improve the solubility and dissolution profile of drugs, various methods have been investigated so far. The cyclodextrin (CD) complexation and phospholipid (PL) complexation are among the exhaustively investigated methods employed for more precise improvement of the solubility and dissolution of poorly water-soluble drugs.
The article discusses the CD and PL complexation techniques of solubility and dissolution enhancement. Various studies reporting the CD and PL complexation as the potential approaches to improve the dissolution, absorption and the bioavailability of the drugs have been discussed. The article critically reviews the physicochemical properties of CDs and PLs, eligibility of drugs for both the complexation, thermodynamics of complexation, methods of preparation, characterization, advantages, limitation and the meta-analysis of some studies for both the techniques.
The CD and PL complexation techniques are very useful in improving solubility and dissolution (and hence the bioavailability) of biopharmaceutical classification system Class II and Class IV drugs. The selection of a particular kind of complexation can be made on the basis of eligibility criteria (of drugs) for the individual techniques, cost, stability and effectiveness of the complexes.
药物的低溶解度和溶出度是药物制剂和给药过程中的主要挑战。为了改善药物的溶解度和溶出度,目前已经研究了各种方法。环糊精(CD)络合和磷脂(PL)络合是为更精确地改善难溶性药物的溶解度和溶出度而进行了详尽研究的方法。
本文讨论了提高溶解度和溶出度的CD和PL络合技术。讨论了各种将CD和PL络合作为改善药物溶出度、吸收和生物利用度的潜在方法的研究。本文批判性地综述了CD和PLs的物理化学性质、两种络合的药物适用性、络合的热力学、制备方法、表征、优点、局限性以及对这两种技术的一些研究的荟萃分析。
CD和PL络合技术在改善生物药剂学分类系统II类和IV类药物的溶解度和溶出度(进而提高生物利用度)方面非常有用。可以根据(药物的)个体技术适用性标准、成本、络合物的稳定性和有效性来选择特定类型的络合。