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| Preparation and evaluation of gestodene loaded microneedles for contraceptive |
| National Research Institute for Family Planning, Beijing, 100081 |
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Abstract To optimize the formulation and preparation technology of gestodene loaded microneedles for contraceptive, and to evaluate the in vitro characteristic of the gestodene loaded microneedles. Methods: The mold casting technique was used to prepare the gestodene loaded microneedles. The matrix materials of these microneedles were selected based on their needle-forming ability and the flexibility. The influence of the adding sample volume and the vacuum drying time on the morphology of the microneedles was researched during the preparation process. The solubility, the puncture performance, the mechanical strength and the in vitro transdermal release behavior of the microneedles were evaluated. Results: Because of the good formation and the certain flexibility, 100 mg/ml PVPK90 was preferred as the optimal matrix solution. The optimal preparation process of the gestodene loaded microneedles included the adding sample volume of 150μl and the vacuum dry of 45 minutes. The gestodene loaded microneedles had certain mechanical strength, which could penetrate the stratum corneum of the porcine skin. The in vitro gestodene release amount of the microneedles was approximately 20μg/cm2 for 7 days consecutively, and which was best fitted by the Higuchi model. The dissolution process of the gestodene loaded microneedles after piercing into the rat skin was evaluated, and the result showed that the microneedles were almost dissolved within 2 min. Conclusion: The preparation method of the gestodene loaded microneedles is simple and the microneedles can slow release gestodene for contraception, and which provides a novel and convenient route for the subcutaneous sustained release contraceptive.
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