Koppisetti HariPriya, Abdella Sadikalmahdi, Nakmode Deepa D, Abid Fatima, Afinjuomo Franklin, Kim Sangseo, Song Yunmei, Garg Sanjay
Centre for Pharmaceutical Innovation, Clinical and Health Sciences, University of South Australia, Adelaide, SA 5000, Australia.
Pharmaceutics. 2025 May 8;17(5):626. doi: 10.3390/pharmaceutics17050626.
Long-acting injectable (LAI) formulations have revolutionized veterinary pharmaceuticals by improving patient compliance, minimizing dosage frequency, and improving therapeutic efficacy. These formulations utilize advanced drug delivery technologies, including microspheres, liposomes, oil solutions/suspensions, in situ-forming gels, and implants to achieve extended drug release. Biodegradable polymers such as poly(lactic--glycolic acid) (PLGA), and polycaprolactone (PCL) have been approved by the USFDA and are widely employed in the development of various LAIs, offering controlled drug release and minimizing the side effects. Various classes of veterinary medicines, including non-steroidal anti-inflammatory drugs (NSAIDs), antibiotics, and reproductive hormones, have been successfully formulated as LAIs. Some remarkable LAI products, such as ProHeart (moxidectin), Excede (ceftiofur), and POSILACTM (recombinant bovine somatotropin), show clinical relevance and commercial success. This review provides comprehensive information on the formulation strategies currently being used and the emerging technologies in LAIs for veterinary purposes. Additionally, challenges in characterization, in vitro testing, in vitro in vivo correlation (IVIVC), and safety concerns regarding biocompatibility are discussed, along with the prospects for next-generation LAIs. Continued advancement in the field of LAI in veterinary medicine is essential for improving animal health.
长效注射（LAI）制剂通过提高患者依从性、减少给药频率和提高治疗效果，彻底改变了兽用药物。这些制剂利用先进的药物递送技术，包括微球、脂质体、油溶液/悬浮液、原位形成凝胶和植入物来实现药物的长效释放。聚（乳酸-乙醇酸）（PLGA）和聚己内酯（PCL）等可生物降解聚合物已获得美国食品药品监督管理局（USFDA）的批准，并广泛应用于各种长效注射制剂的开发中，可实现药物的控释并将副作用降至最低。包括非甾体抗炎药（NSAIDs）、抗生素和生殖激素在内的各类兽用药物已成功制成长效注射制剂。一些著名的长效注射制剂产品，如ProHeart（莫西菌素）、Excede（头孢噻呋）和POSILACTM（重组牛生长激素），显示出临床相关性和商业上的成功。本综述提供了有关目前正在使用的制剂策略以及兽用长效注射制剂中新兴技术的全面信息。此外，还讨论了表征、体外测试、体外-体内相关性（IVIVC）以及生物相容性方面的安全问题，以及下一代长效注射制剂的前景。兽用长效注射制剂领域的持续进步对于改善动物健康至关重要。
