Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest

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 soluti...

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Main Authors: Dongbo Li, Awn Abbas, Nanxin Li, Chao Li, Xiaoyang Ai, Lian Chen, Dongmei Dai, Gang Shu, Juchun Lin, Wei Zhang, Guangneng Peng, Haohuan Li, Funeng Xu, Hualin Fu
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Gels
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Online Access:https://www.mdpi.com/2310-2861/10/12/847
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author Dongbo Li
Awn Abbas
Nanxin Li
Chao Li
Xiaoyang Ai
Lian Chen
Dongmei Dai
Gang Shu
Juchun Lin
Wei Zhang
Guangneng Peng
Haohuan Li
Funeng Xu
Hualin Fu
author_facet Dongbo Li
Awn Abbas
Nanxin Li
Chao Li
Xiaoyang Ai
Lian Chen
Dongmei Dai
Gang Shu
Juchun Lin
Wei Zhang
Guangneng Peng
Haohuan Li
Funeng Xu
Hualin Fu
author_sort Dongbo Li
collection DOAJ
description 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 <sub>(0–∞)</sub> of the altrenogest gel was almost double that of the altrenogest solution. The MRT <sub>(0–∞)</sub> was 40.92 ± 7.21 h and the t<sub>1/2</sub> 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.
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spelling doaj-art-c88def4cc80940819e8afd02f1ca3a4e2025-08-20T02:53:43ZengMDPI AGGels2310-28612024-12-01101284710.3390/gels10120847Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of AltrenogestDongbo Li0Awn Abbas1Nanxin Li2Chao Li3Xiaoyang Ai4Lian Chen5Dongmei Dai6Gang Shu7Juchun Lin8Wei Zhang9Guangneng Peng10Haohuan Li11Funeng Xu12Hualin Fu13Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaDepartment of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu 611130, ChinaAltrenogest 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 <sub>(0–∞)</sub> of the altrenogest gel was almost double that of the altrenogest solution. The MRT <sub>(0–∞)</sub> was 40.92 ± 7.21 h and the t<sub>1/2</sub> 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.https://www.mdpi.com/2310-2861/10/12/847altrenogestgelsviscosity changesustained releasepharmacokinetic
spellingShingle Dongbo Li
Awn Abbas
Nanxin Li
Chao Li
Xiaoyang Ai
Lian Chen
Dongmei Dai
Gang Shu
Juchun Lin
Wei Zhang
Guangneng Peng
Haohuan Li
Funeng Xu
Hualin Fu
Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest
Gels
altrenogest
gels
viscosity change
sustained release
pharmacokinetic
title Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest
title_full Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest
title_fullStr Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest
title_full_unstemmed Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest
title_short Injectable and In Situ Phospholipid-Based Phase Separation Gel for Sustained Delivery of Altrenogest
title_sort injectable and in situ phospholipid based phase separation gel for sustained delivery of altrenogest
topic altrenogest
gels
viscosity change
sustained release
pharmacokinetic
url https://www.mdpi.com/2310-2861/10/12/847
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