Formulation of 99mTechnetium-labeled leuprolide loaded liposomes and its biodistribution study in New Zealand white female rabbits for assessment of its uterine targeting efficiency

Arpita A Patel, Arpita Patel, Amit Tyagi, Rakesh Kumar Sharma, Hetal Thakkar
Drug delivery and translational research · 2017 · vol. 8(1) , pp. 43–53 · doi:10.1007/s13346-017-0432-1 · PMID:29079916 · W2766879119
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⚙ AI-generated summary by claude@2026-06+body, 2026-06-07 ⓘ

99mTc-labeled leuprolide-loaded liposomes administered vaginally showed preferential uterine uptake and retention in rabbits, suggesting improved uterine targeting compared to the plain drug.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-07 ⓘ

The paper studied formulation and characterization of vaginally administered leuprolide acetate–loaded liposomes labeled with 99mTechnetium to assess uterine targeting efficiency. Using a thin-film hydration method with DSPC:cholesterol lipids, the authors measured vesicle size (~189 nm), zeta potential, drug entrapment/loading (74.36% entrapment; 9.29% w/w loading), radiolabeling efficiency/stability, and release over 5 days, and evaluated labeling stability via DTPA challenge and biodistribution by gamma scintigraphy in New Zealand white female rabbits. The liposomes showed sustained release, high 99mTc labeling efficiency and stability in saline/serum, low transchelation, and preferential uterine uptake with longer retention than plain drug. Limitations include that the biodistribution and targeting were assessed only in rabbits and not in human disease models of uterine pathology. This paper is centrally about endometriosis — it investigates uterine targeting of leuprolide acetate, a drug of choice for endometriosis, using an intravaginal delivery strategy aimed at the uterus.

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MeSH descriptors

Leuprolide Technetium Uterus Animals Drug Liberation Female Leuprolide Leuprolide Liposomes Rabbits Technetium Technetium Tissue Distribution Uterus

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