Mahar Riya, Chakraborty Arpita, Nainwal Nidhi, Bahuguna Richa, Sajwan Meenakshi, Jakhmola Vikash
School of Pharmaceutical Sciences, Sardar Bhagwan Singh University, Balawala, Dehradun, 248001, Uttarakhand, India.
Uttaranchal Institute of Pharmaceutical Sciences, Uttaranchal University, Premnagar, Dehradun, 248007, Uttarakhand, India.
AAPS PharmSciTech. 2023 Jan 18;24(1):39. doi: 10.1208/s12249-023-02502-1.
Pulmonary administration of biodegradable polymeric formulation is beneficial in the treatment of various respiratory diseases. For respiratory delivery, the polymer must be non-toxic, biodegradable, biocompatible, and stable. Poly D, L-lactic-co-glycolic acid (PLGA) is a widely used polymer for inhalable formulations because of its attractive mechanical and processing characteristics which give great opportunities to pharmaceutical industries to formulate novel inhalable products. PLGA has many pharmaceutical applications and its biocompatible nature produces non-toxic degradation products. The degradation of PLGA takes place through the non-enzymatic hydrolytic breakdown of ester bonds to produce free lactic acid and glycolic acid. The biodegradation products of PLGA are eliminated in the form of carbon dioxide (CO) and water (HO) by the Krebs cycle. The biocompatible properties of PLGA are investigated in various in vivo and in vitro studies. The high structural integrity of PLGA particles provides better stability, excellent drug loading, and sustained drug release. This review provides detailed information about PLGA as an inhalable grade polymer, its synthesis, advantages, physicochemical properties, biodegradability, and biocompatible characteristics. The important formulation aspects that must be considered during the manufacturing of inhalable PLGA formulations and the toxicity of PLGA in the lungs are also discussed in this paper. Additionally, a thorough overview is given on the application of PLGA as a particulate carrier in the treatment of major respiratory diseases, such as cystic fibrosis, lung cancer, tuberculosis, asthma, and pulmonary hypertension.
可生物降解聚合物制剂的肺部给药在各种呼吸道疾病的治疗中具有益处。对于呼吸道给药，聚合物必须无毒、可生物降解、具有生物相容性且稳定。聚D，L-乳酸-乙醇酸共聚物（PLGA）是一种广泛用于可吸入制剂的聚合物，因为其具有吸引人的机械和加工特性，这为制药行业提供了大量机会来开发新型可吸入产品。PLGA有许多药物应用，其生物相容性会产生无毒的降解产物。PLGA的降解通过酯键的非酶促水解断裂来进行，生成游离乳酸和乙醇酸。PLGA的生物降解产物通过三羧酸循环以二氧化碳（CO）和水（HO）的形式被清除。PLGA的生物相容性特性在各种体内和体外研究中得到了探究。PLGA颗粒的高度结构完整性提供了更好的稳定性、出色的药物负载能力和持续的药物释放。本综述提供了关于PLGA作为可吸入级聚合物的详细信息，包括其合成、优点、物理化学性质、生物可降解性和生物相容性特征。本文还讨论了在制造可吸入PLGA制剂过程中必须考虑的重要制剂方面以及PLGA在肺部的毒性。此外，还对PLGA作为颗粒载体在治疗主要呼吸道疾病（如囊性纤维化、肺癌、肺结核、哮喘和肺动脉高压）中的应用进行了全面概述。
