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Exploring Trehalose on the Release of Levonorgestrel from Implantable PLGA Microneedles.

ABSTRACT: Hydrophobic drugs wrapped in poly (lactic-co-glycolic acid) (PLGA)-based microneedles (MNs) require a long time to release completely. To obtain the desired duration, it is still necessary to modulate the release of hydrophobic drugs from MNs, while the PLGA composition is unchangeable. In this work, implantable PLGA microneedles (IPMNs) composed of PLGA arrowheads encapsulating levonorgestrel (LNG) and a water-soluble supporting array were designed. We explored trehalose used as a porogen on the release of hydrophobic LNG from PLGA-based MNs. Varying the trehalose content in PLGA arrowheads could induce different rates of drug release. The highest cumulative release of LNG was 76.2 ± 3.9% for IPMNs with 33.3% trehalose during 21 days in vitro, while the cumulative release of LNG was 60.4 ± 3.5% for IPMNs without trehalose. Pharmacokinetic results in rats showed that plasma levels of LNG were sustained for 13 days for IPMNs with 33.3% trehalose and 16 days for IPMNs without trehalose. Furthermore, the PLGA arrowheads with trehalose degraded more rapidly than those without trehalose over 21 days in rats. Consequently, using trehalose as a porogen was a feasible approach to modulate the release of a hydrophobic drug from PLGA-based MNs.

SUBMITTER: Zhao X

PROVIDER: S-EPMC7023614 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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Exploring Trehalose on the Release of Levonorgestrel from Implantable PLGA Microneedles.

Zhao Xiaoyu X Zhang Suohui S Yang Guozhong G Zhou Zequan Z Gao Yunhua Y

Polymers 20200101 1

Hydrophobic drugs wrapped in poly (lactic-co-glycolic acid) (PLGA)-based microneedles (MNs) require a long time to release completely. To obtain the desired duration, it is still necessary to modulate the release of hydrophobic drugs from MNs, while the PLGA composition is unchangeable. In this work, implantable PLGA microneedles (IPMNs) composed of PLGA arrowheads encapsulating levonorgestrel (LNG) and a water-soluble supporting array were designed. We explored trehalose used as a porogen on th ...[more]

PMID: 31906331

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Project description:ObjectiveThe objective was to characterize and compare in vivo rates of levonorgestrel (LNG) release from Sino-implant (II) and Jadelle® contraceptive implants.Study designWe sampled 48 Sino-implant (II) and 49 Jadelle® explant sets for residual LNG content from participants treated for up to 51 months in a randomized contraceptive efficacy trial in the Dominican Republic (DR). Additional Sino-implant (II) explants were obtained from 8 women who became pregnant in the DR trial and 10 who contributed 3 to 5 years of use in a cohort study in China. Baseline LNG loads were estimated from five unused implant sets per device type. Release profiles were estimated using mixture models that captured initial burst fractions and compared with efficacy and pharmacokinetics data from the DR trial.ResultsEstimated baseline LNG loads for Sino-implant (II) and Jadelle® were 142.8 mg and 150.5 mg, respectively (vs. the labeled 150 mg). There was an initial burst release of drug (5.6% and 7.9%, respectively) followed by an exponential decrease in LNG content evident for each device. Release rates were significantly lower for Sino-implant (II) throughout the treatment period, with estimated rates after 3 years of 24.2 mcg/day and 29.0 mcg/day for Sino-implant (II) and Jadelle®, respectively. The estimated Sino-implant (II) rate after 3 years was similar to the predicted rate after 5 years (23.6 mcg/day) for Jadelle® (rate ratio: 1.03; 95% confidence interval: 0.92-1.13).ConclusionsSino-implant (II) LNG release rates were significantly lower than Jadelle® with Sino-implant (II) rates through year 3 comparable to Jadelle® rates through year 5. These results reinforce the 3-year duration of action for which Sino-implant (II) was prequalified by the World Health Organization.ImplicationsThis analysis confirms the WHO prequalification of Sino-implant (II) for 3 years of use and supports different durations of action for Jadelle® and Sino-implant (II). It provides additional evidence that this approach can complement efficacy trials in determining duration of action of hormonal contraceptives in general.

Dataset Information

Exploring Trehalose on the Release of Levonorgestrel from Implantable PLGA Microneedles.

Publications

Exploring Trehalose on the Release of Levonorgestrel from Implantable PLGA Microneedles.

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