Dinh Linh, Blackard Jason T, Robertson Jaime, Atreya Abby, Horner Shaina, Brown Jennifer L, Gomez Luis A, Beegle Stephen, Mahon Lanesa, Eades William, Abdolmohammadpourbonab Shayan, Liu William, Meeds Heidi L, Fedders Kevin, Twitty T Dylanne, Welge Jeffrey A, Yan Bingfang
Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH 45229, USA.
Division of Digestive Diseases, Department of Internal Medicine, University of Cincinnati College of Medicine, Cincinnati, OH 45229 USA; Center for Addiction Research, University of Cincinnati College of Medicine, Cincinnati, OH 45219, USA.
Int J Pharm. 2025 Feb 10;670:125157. doi: 10.1016/j.ijpharm.2024.125157. Epub 2024 Dec 31.
Conventional drug formulations release active pharmaceutical ingredients (APIs) immediately after administration, while long-acting (LA) drug products are designed for prolonged therapeutic effects, thereby reducing administration frequency and improving patient compliance. The development of LA therapeutics for chronic disease treatment has significantly helped patients adhere to their regimens, reducing the need for daily doses and easing the burden on healthcare systems. Advances in treatment have transformed Human Immunodeficiency Virus (HIV) into a manageable chronic disease, and efforts are underway to eliminate HIV in the future. Nowadays, antiretroviral therapies (ARTs) are widely available and accessible, daily oral pre-exposure prophylaxis (PrEP) has been highly effective and the new LA ARTs and LA PrEP are being actively pursued. The development of LA antiretrovirals for HIV has revolutionized the landscape of global implementation of HIV prevention and treatment. This article provides an overview of LA medicines (pills, injections, solid implants, and in situ forming depots) for the prevention and treatment of HIV from a pharmaceutics perspective, describing approved medicines, recognizing promising technologies, and discussing the pros and cons of poly (lactic-co-glycolic acid) (PLGA) particles, liposomes, hydrogels, and organogel formulations.
传统药物制剂在给药后会立即释放活性药物成分（API），而长效（LA）药物产品则旨在实现延长的治疗效果，从而减少给药频率并提高患者依从性。用于慢性病治疗的长效疗法的发展显著帮助患者坚持治疗方案，减少每日剂量需求并减轻医疗系统负担。治疗方面的进展已将人类免疫缺陷病毒（HIV）转变为一种可控制的慢性病，并且正在努力在未来消除HIV。如今，抗逆转录病毒疗法（ART）广泛可得且易于获取，每日口服暴露前预防（PrEP）已非常有效，新型长效抗逆转录病毒疗法和长效PrEP正在积极研发中。用于HIV的长效抗逆转录病毒药物的开发彻底改变了全球HIV预防和治疗的实施格局。本文从药剂学角度概述了用于HIV预防和治疗的长效药物（片剂、注射剂、固体植入剂和原位形成贮库），描述了已批准的药物，认识到有前景的技术，并讨论了聚（乳酸-乙醇酸）（PLGA）颗粒、脂质体、水凝胶和有机凝胶制剂的优缺点。
