Li Dongbo, Abbas Awn, Li Nanxin, Li Chao, Ai Xiaoyang, Chen Lian, Dai Dongmei, Shu Gang, Lin Juchun, Zhang Wei, Peng Guangneng, Li Haohuan, Xu Funeng, Fu Hualin
Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, China.
Gels. 2024 Dec 23;10(12):847. doi: 10.3390/gels10120847.
Altrenogest is a key regulatory hormone for intensive and batch management of reserve sows in breeding farms. As a synthetic hormone, altrenogest could make ovaries stay at the initial stage of follicles and inhibit estrus and ovulation in animals. However, the currently used oral altrenogest solution needs to be administered continuously every day for more than two weeks in clinical practice. In this study we developed a phospholipid-based injectable gel carrying altrenogest to decrease the number of administrations, sustain release of the drug, and enhance therapeutic efficacy for clinical use. The altrenogest gel had a viscosity of 100 cP before phase transition and over 1,000,000 cP after phase transition. In vitro, altrenogest can be continuously released from gel for over two weeks. The pharmacokinetic results showed that the AUC of the altrenogest gel was almost double that of the altrenogest solution. The MRT was 40.92 ± 7.21 h and the t of the altrenogest gel was 80.03 ± 20.79 h. The altrenogest gel demonstrated excellent fluidity, ease of injectability, high drug-loading capacity, and appropriate sustained-release characteristics both in vitro and in vivo, making it a potential drug delivery system for swine production.
烯丙孕素是养殖场后备母猪集约化和批次化管理的关键调控激素。作为一种合成激素，烯丙孕素可使卵巢停留在卵泡初始阶段，抑制动物发情和排卵。然而，目前临床使用的口服烯丙孕素溶液在实践中需要每天连续给药两周以上。在本研究中，我们开发了一种载有烯丙孕素的磷脂基可注射凝胶，以减少给药次数、实现药物缓释并提高临床治疗效果。烯丙孕素凝胶在相变前粘度为100厘泊，相变后超过1,000,000厘泊。在体外，烯丙孕素可从凝胶中持续释放两周以上。药代动力学结果表明，烯丙孕素凝胶的AUC几乎是烯丙孕素溶液的两倍。烯丙孕素凝胶的MRT为40.92±7.21小时，t为80.03±20.79小时。烯丙孕素凝胶在体外和体内均表现出优异的流动性、易于注射、高载药量和适当的缓释特性，使其成为猪生产中一种潜在的药物递送系统。
