A new long-acting injectable microcapsule system for the administration of progesterone.
A long-acting injectable microcapsule system for the controlled-release systemic administration of progesterone (P4) is described. The system consists of microcapsules made of the biodegradable polymer, d,l-polylactic acid, which contain crystalline P4. Following injection, P4 is released from the microcapsules by diffusion and biodegradation of the polymer matrix. The rate of P4 release from the prototype microcapsule system in vivo is 1.3 microgram of P4/day/mg of microcapsules, and the duration of release is 30 days. Vaginal estrous cycles in rats and cyclic ovarian function in baboons were inhibited for 1 month following a single injection of P4 microcapsules. The effects of continuous progesterone therapy on reproductive function in both rats and baboons are dose-dependent. The utility of the system as a once-a-month injectable contraceptive is established in the baboon model.
D000818:Animals; D003270:Contraceptive Agents / Q000008:administration & dosage*; D003692:Delayed-Action Preparations; D004353:Drug Evaluation, Preclinical; D005260:Female; D007273:Injections, Intramuscular; D007773:Lactates; D008863:Microspheres; D010215:Papio; D011108:Polymers; D011374:Progesterone / Q000008:administration & dosage*; D051381:Rats
D003270:Contraceptive Agents; D003692:Delayed-Action Preparations; D007773:Lactates; D011108:Polymers; D011374:Progesterone