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Updated: Apr 30, 2026

Encapsulated Cell Technology for the Delivery of Biologics to the Mouse Eye
Published on: March 30, 2020
A new injectable liquid crystal system for one month delivery of leuprolide
Min-Hyo Ki1, Jong-Lae Lim2, Jin-Young Ko3
1Chong Kun Dang Research Institute, CKD Pharmaceuticals Inc., 464-3 Jung-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-916, Republic of Korea; College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Republic of Korea.
Abstract:
An injectable liquid crystal-forming system (LCFS) was prepared by using sorbitan monooleate (SMO) as a new liquid crystal-forming material for injections, and its potential use of clinically available sustained-release formulation was evaluated. LCFS was prepared using SMO mixed with phosphatidyl choline and tocopherol acetate, and contained 3.75 mg of leuprolide acetate as a monthly dose in 90 μl in liquid form. The semi-solid mesophase was formed from the liquid LCFS when it contacted water. The mesophase showed typical characteristics of the liquid crystalline phase, which was classified as the hexagonal phase. The safety of the LCFS was studied by an in vitro extraction colony assay and by examining the injection site in rats and white rabbits after an autopsy. Both in vitro release test and in vivo pharmacokinetic and pharmacodynamic studies showed a sustained release of leuprolide. When compared with a commercial depot formulation of leuprolide, the LCFS showed a similar AUClast value and significantly reduced initial burst with sufficient suppression of testosterone after subcutaneous injections in rats and dogs. The LCFS can serve as a new type of sustained-release injection formulation for its safety, ease of preparation, and sustained release properties.
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