Acarbose-Loaded PLGA Microspheres: Efficient Encapsulation and Controlled Release
Abstract
Acarbose, a locally administered oral anti-diabetic agent, also experiences bioavailability and controlled release difficulties. To overcome such limitations, Acarbose-loaded microspheres were designed to ensure a higher therapeutic efficacy through controlled release of the drug and increased stability. Microspheres were prepared using the solvent evaporation process with different ratios of drug and polymer. The best drug release profile was selected, and optimization of the formulation was done further. Encapsulation efficiency, particle size, surface topography, and drug release rates were considered critical parameters to test. Characterization of the microspheres was conducted through Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FTIR) to determine morphology, drug-polymer interaction, and physical state of Acarbose. Particle size distribution and zeta potential were also investigated to determine the stability of the formulation. The microspheres obtained using a 1:4 (Acarbose: PLGA) ratio showed high encapsulation efficiency (95.7%) and sustained release of drug for 24 hours. The optimized formulation showed smooth spherical morphology, particle size of 165.4 µm, and good flow properties. The zeta potential of the formulation showed excellent dispersion stability. The findings indicate that the 1:4 Acarbose: PLGA microspheres offer a promising drug delivery system with controlled release, improved stability, and good dispersion characteristics. These results underscore the possibility of enhancing the bioavailability and therapeutic activity of Acarbose, opening the door for additional in vivo investigations and clinical use.
Keywords: Acarbose, microspheres, solvent evaporation, PLGA, drug release, encapsulation efficiency, particle size distribution, zeta potential, SEM, DSC, FTIR, drug delivery system.
Keywords:
Acarbose, microspheres, solvent evaporation, PLGA, drug release, encapsulation efficiencyDOI
https://doi.org/10.22270/jddt.v15i6.7165References
1. Bhagavan NV, Ha CE. Perturbations of Energy Metabolism. In: Essentials of Medical Biochemistry. Elsevier; 2011:261-274. doi:10.1016/B978-0-12-095461-2.00020-5 https://doi.org/10.1016/B978-0-12-095461-2.00020-5
2. Dilworth L, Facey A, Omoruyi F. Diabetes Mellitus and Its Metabolic Complications: The Role of Adipose Tissues. IJMS. 2021;22(14):7644. https://doi.org/10.3390/ijms22147644 PMid:34299261 PMCid:PMC8305176
3. Gonzalez-Freire M, Diaz-Ruiz A, Hauser D, et al. The road ahead for health and lifespan interventions. Ageing Research Reviews. 2020;59:101037. https://doi.org/10.1016/j.arr.2020.101037 PMid:32109604 PMCid:PMC7450388
4. Garber AJ. Anti-Obesity Pharmacotherapy and the Potential for Preventing Progression from Prediabetes to Type 2 Diabetes. Endocrine Practice. 2015;21(6):634-644. https://doi.org/10.4158/EP14460.RA PMid:25716632
5. Adepu S, Ramakrishna S. Controlled Drug Delivery Systems: Current Status and Future Directions. Molecules. 2021;26(19):5905. https://doi.org/10.3390/molecules26195905 PMid:34641447 PMCid:PMC8512302
6. Ezike TC, Okpala US, Onoja UL, et al. Advances in drug delivery systems, challenges and future directions. Heliyon. 2023;9(6):e17488. https://doi.org/10.1016/j.heliyon.2023.e17488 PMid:37416680 PMCid:PMC10320272
7. Xu S, Liu Y, Chen Y, Wu G. Efficient Encapsulation and Controlled Release of the Pesticide Emamectin Benzoate in Polylactic Acid Microspheres Prepared by Modified Solvent Evaporation. Molecules. 2024;29(24):6008. https://doi.org/10.3390/molecules29246008 PMid:39770095 PMCid:PMC11677981
8. Su Y, Zhang B, Sun R, et al. PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application. Drug Delivery. 2021;28(1):1397-1418. https://doi.org/10.1080/10717544.2021.1938756 PMid:34184949 PMCid:PMC8248937
9. Lengyel M, Kállai-Szabó N, Antal V, Laki AJ, Antal I. Microparticles, Microspheres, and Microcapsules for Advanced Drug Delivery. Sci Pharm. 2019;87(3):20. https://doi.org/10.3390/scipharm87030020
10. Sherrington LA, Sherrington A. Guaifenesin. In: Analytical Profiles of Drug Substances and Excipients. Vol 25. Elsevier; 1998:121-164. https://doi.org/10.1016/S0099-5428(08)60754-6
11. Gaikwad SS, Kothule AM, Morade YY, et al. An overview of the implementation of SeDeM and SSCD in various formulation developments. International Journal of Pharmaceutics. 2023;635:122699. https://doi.org/10.1016/j.ijpharm.2023.122699 PMid:36764417
12. Teferra TF. Engineering Properties of Food Materials. In: Handbook of Farm, Dairy and Food Machinery Engineering. Elsevier; 2019:45-89. https://doi.org/10.1016/B978-0-12-814803-7.00003-8
13. Kaur A. 86 PUBLICATIONS 1,462 CITATIONS SEE PROFILE. Published online 2013.
14. Mukherjee PK, Harwansh RK, Bhattacharyya S. Bioavailability of Herbal Products. In: Evidence-Based Validation of Herbal Medicine. Elsevier; 2015:217-245. https://doi.org/10.1016/B978-0-12-800874-4.00010-6
15. Varenne F, Coty JB, Botton J, et al. Evaluation of zeta potential of nanomaterials by electrophoretic light scattering: Fast field reversal versus Slow field reversal modes. Talanta. 2019;205:120062. https://doi.org/10.1016/j.talanta.2019.06.062 PMid:31450425
16. Yang Y, Gao Y, Mei X. Effects of formulation parameters on encapsulation efficiency and release behavior of thienorphine loaded PLGA microspheres. Pharmaceutical Development and Technology. 2013;18(5):1169-1174. https://doi.org/10.3109/10837450.2011.618948 PMid:21967467
17. El-Say KM. Maximizing the encapsulation efficiency and the bioavailability of controlled-release cetirizine microspheres using Draper–Lin small composite design. DDDT. Published online February 2016:825. https://doi.org/10.2147/DDDT.S101900 PMid:26966353 PMCid:PMC4771436
18. Gaba P, Singh S, Gaba M, Gupta GD. Galactomannan gum coated mucoadhesive microspheres of glipizide for treatment of type 2 diabetes mellitus: In vitro and in vivo evaluation. Saudi Pharmaceutical Journal. 2011;19(3):143-152. https://doi.org/10.1016/j.jsps.2011.02.001 PMid:23960752 PMCid:PMC3745188
19. Kumar A, Sharma AK, Dutt R. A Review of gastro-retentive drug delivery systems for antidiabetics and its present status. RESEARCH JOURNAL OF PHARMACY AND TECHNOLOGY. 2021;14(1):538-546. https://doi.org/10.5958/0974-360X.2021.00098.6
20. Zhu W, Long J, Shi M. Release Kinetics Model Fitting of Drugs with Different Structures from Viscose Fabric. Materials. 2023;16(8):3282. https://doi.org/10.3390/ma16083282 PMid:37110118 PMCid:PMC10146738
21. Mailafiya MM, Abubakar K, Danmaigoro A, et al. Evaluation of in vitro release kinetics and mechanisms of curcumin-loaded cockle shell-derived calcium carbonate nanoparticles. Biomed Res Ther. 2019;6(12):3518-3540. https://doi.org/10.15419/bmrat.v6i12.580
22. González-González O, Ramirez IO, Ramirez BI, et al. Drug Stability: ICH versus Accelerated Predictive Stability Studies. Pharmaceutics. 2022;14(11):2324. https://doi.org/10.3390/pharmaceutics14112324 PMid:36365143 PMCid:PMC9693625
23. PHARMACEUTICAL STABILITY STUDIES AND THEIR REGULATORY SUBMISSION REQUIREMENTS: A REVIEW. IJBPAS. 2024;13(8). https://doi.org/10.31032/IJBPAS/2024/13.8.8257
24. Pavčnik L, Prunk M, Trdan Lušin T, Roškar R. Accelerated Predictive Stability Testing: Accelerating Registration Phase and Application of Reduced Designs for Shelf-Life Determination of Parenteral Drug Product. Pharmaceutics. 2025;17(2):160. https://doi.org/10.3390/pharmaceutics17020160 PMid:40006527 PMCid:PMC11858995
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Copyright (c) 2025 Anurag Mishra , Suresh Waghamare , S. G. Khanage

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