An update on Nanoparticle Formulation Design of Piperine to Improve its Oral bioavailability: A Review

A. Nugroho, Nindya Kusumorini, S. Pramono, R. Martien
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Abstract

Piperine, a crystalline alkaloid compound isolated from Piper nigrum, piper longum, and other types of piper, has had many fabulous pharmacological advantages for preventing and treating some specific diseases, such as analgesic, anti-inflammatory, hepatoprotective, antimetastatic, antithyroid, immunomodulatory, antitumor, rheumatoid arthritis, osteoarthritis, Alzheimer's, and improving the bioavailability of other drugs. However, its potential for clinical use through oral usage is hindered by water solubility and poor bioavailability. The low level of oral bioavailability is caused by low solubility in water and is photosensitive, susceptible to isomerization by UV light, which causes piperine concentration to decrease. Many different formulation approaches have been applied to improve the poor oral bioavailability of piperine. There have been oral formulation strategies that have been successfully implemented in increasing the solubility and bioavailability of piperine within the body, such as the formulation of nanoparticles, nanosuspensions, salt formation, liposomes, complexation using polymers, micro/nano-emulsions, and solid dispersions. This review presents a summary of piperine biopharmaceuticals, new formulation design approaches to improve oral bioavailability of piperine, and several techniques and methods for conducting selective and sensitive analysis of piperine in biological fluids.
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提高胡椒碱口服生物利用度的纳米颗粒配方设计研究进展
胡椒碱是一种从黑椒、长椒和其他类型的胡椒中分离出来的结晶生物碱化合物,在预防和治疗一些特定疾病方面具有许多令人难以相信的药理优势,如镇痛、抗炎、保肝、抗转移、抗甲状腺、免疫调节、抗肿瘤、类风湿关节炎、骨关节炎、阿尔茨海默氏症,以及提高其他药物的生物利用度。然而,由于水溶性和较差的生物利用度,其通过口服应用于临床的潜力受到阻碍。口服生物利用度低是由于在水中的溶解度低,并且具有光敏性,容易受到紫外线的异构化,从而导致胡椒碱浓度降低。许多不同的配方方法已被应用于改善胡椒碱的口服生物利用度差。已经有一些口服配方策略成功地提高了胡椒碱在体内的溶解度和生物利用度,例如纳米颗粒、纳米悬浮液、盐形成、脂质体、聚合物络合、微/纳米乳液和固体分散体的配方。本文综述了胡椒碱生物制药、提高胡椒碱口服生物利用度的新剂型设计方法,以及生物体液中胡椒碱选择性和敏感性分析的几种技术和方法。
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