Research Institute for Medicines and Pharmaceutical Sciences, Faculty of Pharmacy, University of Lisbon, Portugal.
AAPS PharmSciTech. 2011 Dec;12(4):1276-92. doi: 10.1208/s12249-011-9690-2. Epub 2011 Sep 27.
Cyclodextrins (CDs) are used in oral pharmaceutical formulations, by means of inclusion complexes formation, with the following advantages for the drugs: (1) solubility, dissolution rate, stability, and bioavailability enhancement; (2) to modify the drug release site and/or time profile; and (3) to reduce or prevent gastrointestinal side effects and unpleasant smell or taste, to prevent drug-drug or drug-additive interactions, or even to convert oil and liquid drugs into microcrystalline or amorphous powders. A more recent trend focuses on the use of CDs as nanocarriers, a strategy that aims to design versatile delivery systems that can encapsulate drugs with better physicochemical properties for oral delivery. Thus, the aim of this work was to review the applications of the CDs and their hydrophilic derivatives on the solubility enhancement of poorly water-soluble drugs in order to increase their dissolution rate and get immediate release, as well as their ability to control (to prolong or to delay) the release of drugs from solid dosage forms, either as complexes with the hydrophilic (e.g., as osmotic pumps) and/or hydrophobic CDs. New controlled delivery systems based on nanotechnology carriers (nanoparticles and conjugates) have also been reviewed.
环糊精（CDs）被用于口服药物制剂中，通过形成包合物，具有以下优点：（1）提高药物的溶解度、溶解速率、稳定性和生物利用度；（2）改变药物释放部位和/或时间曲线；（3）减少或预防胃肠道副作用和不良气味或味道，防止药物-药物或药物添加剂相互作用，甚至将油和液体药物转化为微晶或无定形粉末。最近的一个趋势集中在将 CD 用作纳米载体上，这一策略旨在设计多功能的给药系统，能够封装具有更好理化性质的药物，用于口服给药。因此，本工作旨在综述 CD 及其亲水性衍生物在提高疏水性药物溶解度方面的应用，以提高其溶解速率和获得即刻释放，并具有控制（延长或延迟）药物从固体剂型中释放的能力，无论是与亲水性（例如，作为渗透压泵）和/或疏水性 CD 形成复合物。还综述了基于纳米技术载体（纳米粒子和缀合物）的新型控释系统。
