制造含有黄体酮自微乳剂的控释聚合物微针,用于透皮给药。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Phuvamin Suriyaamporn, Porawan Aumklad, Theerasak Rojanarata, Prasopchai Patrojanasophon, Tanasait Ngawhirunpat, Boonnada Pamornpathomkul, Praneet Opanasopit
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引用次数: 0

摘要

孕酮(PG)已被批准用于激素替代疗法,以降低子宫内膜癌的风险。然而,由于黄体酮降解快,口服黄体酮的疗效不佳。透皮孕酮具有一定优势,但由于其溶解度较低(Log P = 3.9)而缺乏疗效。因此,本研究旨在评估自微乳化给药系统(SMEDDS)与聚合物微针(MNs)的结合如何以控释方式改善 PG 的透皮给药。在 PG-SMEDDS 中,PG-SME5 因其理想的特性和稳定性而被选中。包含 PG-SME5 的双层聚合物 MNs 制剂(PG-SMEDDS-tMNs)由聚合物水混合物作为第一层,20% PCL 作为第二层配制而成。它成功地渗透了新生猪皮肤,在使用后 15 分钟内观察到第一层溶解。体外皮肤渗透显示,使用 PG-SMEDDS-tMNs 82 小时内渗透皮肤的 PG 百分比高于 PG 悬浮液和 PG-SMEDDS。樋口动力学显示,PG-SMEDDS-tMNs 可在 15 天内控制 PG 的释放。这些研究表明,将 PG-SMEDDS 加入控释双层聚合物 MNs 中可能是改善 PG 透皮给药的一种很有前景的方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Fabrication of controlled-release polymeric microneedles containing progesterone-loaded self-microemulsions for transdermal delivery.

Progesterone (PG) has been approved for hormone replacement therapy to mitigate the risk of endometrial carcinoma. However, there has been a lack of success in oral PG due to its rapid degradation. Transdermal PG has advantages but lacks efficacy due to its poor solubility (Log p = 3.9). Therefore, this study aimed to evaluate how combining self-microemulsifying drug delivery systems (SMEDDS) and polymeric microneedles (MNs) could improve the transdermal delivery of PG in a controlled-release manner. Among PG-SMEDDS, PG-SME5 was selected for its desirable properties and stability. The two-layer polymeric MNs formulation incorporating PG-SME5 (PG-SMEDDS-tMNs) was formulated from aqueous blends of polymers as a first layer and 20% PCL as a second layer. It successfully penetrated neonatal porcine skin with the dissolution of the first layer observed within 15 min after application. In vitro skin permeation revealed that the percentage of PG which permeated the skin over 82 h using PG-SMEDDS-tMNs was higher than a PG-suspension and PG-SMEDDS. The Higuchi kinetic showed controlled release over 15 days of PG from PG-SMEDDS-tMNs. These studies suggested that incorporating PG-SMEDDS into controlled-release two-layer polymeric MNs could be a promising approach for improving the transdermal delivery of PG.

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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
审稿时长
1 months
期刊介绍: Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.
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