Kumamoto University, Graduate School of Medical and Pharmaceutical Sciences, Oe-honmachi, Kumamoto, Japan.
Expert Opin Drug Deliv. 2010 May;7(5):565-75. doi: 10.1517/17425241003713486.
Biodegradable solid particles are potential carriers for both hydrophobic and hydrophilic drugs and have been marketed for prolongation of pharmaceutical activity. In developing such particles, it is important to achieve stable encapsulation of the drugs in the particles and a controlled rate of drug release.
In this paper, the principles and techniques for preparing such particles are reviewed.
Overall, it remains difficult to identify a general approach for achieving effective entrapment and controlled release, because these qualities are determined by multiple complex factors. The encapsulation efficiency of drugs in particles can be improved through various techniques, including hydrophobic interaction, covalent bonding, ionic interaction and physical isolation. In addition, the release behaviors of drugs are strongly influenced by environmental conditions as well as the physicochemical properties of the polymers and drugs.
Solid particles with targeting ability in addition to prolongation of biological activity may have potential for development of a new type of pharmaceutical in the clinical field.
可生物降解的固体颗粒是潜在的载体,既适用于疏水性药物又适用于亲水性药物,并已被推向市场以延长药物的活性。在开发此类颗粒时,重要的是要实现药物在颗粒中的稳定包封和药物的控制释放速率。
本文综述了制备此类颗粒的原理和技术。
总体而言,由于这些特性取决于多个复杂因素,因此仍然难以确定实现有效包封和控制释放的一般方法。通过多种技术可以提高药物在颗粒中的包封效率,包括疏水相互作用、共价键合、离子相互作用和物理隔离。此外,药物的释放行为受环境条件以及聚合物和药物的物理化学性质的强烈影响。
除了延长生物活性之外,具有靶向能力的固体颗粒可能有潜力在临床领域开发新型药物。