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 vitro transdermal 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.
