Title:Design, Synthesis, and Evaluation of Lipoyl Ester Conjugated Star PLGA
for Sustained Drug Delivery Systems
Volume: 7
Issue: 1
Author(s): Akanksha Singh, Chandan Gupta, Shrikant Godse and Rajani Athawale*
Affiliation:
- Prin. K. M. Kundnani College of Pharmacy, Cuffe Parade, Mumbai, 400 005, India
Keywords:
Poly(lactic-co-glycolic acid), star PLGA, lipoyl ester terminated star PLGA, copolymer, tissue engineering, FT-IR.
Abstract:
Background: Poly(lactic-co-glycolic acid) (PLGA), an FDA-approved copolymer, is
widely recognized for its biocompatibility, biodegradability, and versatility in drug delivery systems.
Despite its advantages, challenges, such as poor drug loading and burst release, motivate
the exploration of innovative modifications. The current research aimed to modify the linear
PLGA to lipoyl ester terminated star PLGA polymer to minimize initial burst release by increasing
the molecular weight and fabricate risperidone-loaded microspheres.
Methods: In this study, we have presented a novel approach involving the synthesis of star
PLGA through the direct melt polycondensation of PLGA with pentaerythritol, followed by conjugation
with lipoic acid to form lipoyl ester terminated star PLGA. Structural confirmation was
done by Fourier Transform Infrared spectroscopy (FT-IR), proton Nuclear Magnetic Resonance
(1H-NMR), and Gel Permeation Chromatography (GPC). Microspheres were fabricated from
lipoyl ester terminated star PLGA and characterized for their particle size and surface morphology
by Scanning Electron Microscopy (SEM) and in vitro drug release by dialysis bag method.
Results: The results of the study have indicated successful conjugation of lipoic acid to star
PLGA forming lipoyl ester terminated star PLGA, as confirmed by FT-IR, 1H-NMR, and GPC
analyses. Microspheres developed from the synthesized polymer exhibited particle sizes ranging
from 4.64 μm to 11.7 μm and demonstrated sustained drug delivery, with 99.8% release over 45
d, in contrast to the plain drug that achieved complete dissolution within 3 h.
Conclusion: The resulting material has demonstrated unique bioresponsive and multifunctional
properties, with evidence of successful synthesis provided through comprehensive characterization
techniques, and suitability for the fabrication of microspheres for sustained drug delivery
systems.