Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation

Title:Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation

Volume: 21 Issue: 11

Author(s): Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao*Mingguan Piao*

Affiliation:

• College of Pharmacy, Yanbian University, Yanji, P.R. China

• College of Pharmacy, Yanbian University, Yanji, P.R. China
• Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University, Yanji, P.R. China

Keywords: Linagliptin, transdermal drug delivery systems, microparticle, gel, spray drying method, dual reservoir slow release.

Abstract:

Background: Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.

Objective: The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.

Methods: Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitrotransdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.

Results: The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.

Conclusion: These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.

Cite this article as:

Liu Jiayan, Guo Song, Hong Shuai, Piao Jingshu*, Piao Mingguan*, Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation, Current Drug Delivery 2024; 21 (11) . https://dx.doi.org/10.2174/0115672018279370240103062944