Encapsulation Of Sitagliptin in Polymer-Based Microspheres for Sustained Anti-Diabetic Therapy
Keywords:
Biodegradable Polymers, Controlled Release, Diabetes Mellitus, Drug Delivery System, Encapsulation Efficiency, Microspheres, PLGA, Polymer-Based Delivery, Sitagliptin, Sustained Release, Type 2 Diabetes, Therapeutic EfficacyAbstract
Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is widely used for managing type 2 diabetes mellitus but suffers from a short half-life and requires frequent dosing, which may reduce patient compliance. Encapsulation of sitagliptin in polymer-based microspheres offers a promising approach for sustained anti-diabetic therapy by prolonging drug release, enhancing bioavailability, and improving therapeutic efficacy. Various biodegradable and biocompatible polymers such as albumin, chitosan, hydroxypropyl methylcellulose (HPMC), poly(lactic-co-glycolic acid) (PLGA), and Eudragit have been utilized to fabricate microspheres using techniques like spray-drying, solvent evaporation, and ionic gelation. These microspheres demonstrate favorable micromeritic properties, high drug entrapment efficiency, and controlled drug release kinetics primarily governed by diffusion mechanisms following Higuchi or Peppas models. Mucoadhesive properties of polymers like chitosan and HPMC enhance gastrointestinal residence time, resulting in better drug retention and sustained action in vivo. Studies affirm that sitagliptin-loaded microspheres achieve extended drug release ranging from 12 to 24 hours, reduce dosing frequency, and minimize side effects associated with conventional formulations. This encapsulation strategy thus represents an effective oral drug delivery system with potential to improve glycemic control, patient adherence, and overall clinical outcomes in diabetes management
Downloads
Metrics
References
Revathi, M., & Dhanaraju, M. D. (2018). Formulation and evaluation of Sitagliptin microspheres for the treatment of type 2 diabetes mellitus. Asian Journal of Pharmaceutical and Clinical Research, 11(6), 318–322.
SreeHarsha, N., Dubey, S. K., SanthaLakshmi, G., & Abdul Hasan, S. (2019). Development and characterization of Sitagliptin mucoadhesive nanoparticles for prolonged release. International Journal of Nanomedicine, 14, 3999–4011. https://doi.org/10.2147/IJN.S197393
Nair, A. B., Jacob, S., Al-Dhubiab, B. E., & Attimarad, M. (2019). Formulation and evaluation of mucoadhesive polymeric nanoparticles of Sitagliptin for oral controlled release. Pharmaceuticals, 12(4), 163. https://doi.org/10.3390/ph12040163
Nair, A. B., Jacob, S., Al-Dhubiab, B. E., & Attimarad, M. (2020). Formulation of thiolated chitosan nanoparticles for enhanced oral delivery of Sitagliptin. Pharmaceutics, 12(4), 300. https://doi.org/10.3390/pharmaceutics12040300
Harsha, N. S., Sudheer, P., & Santhosh Kumar, T. R. (2013). Development and evaluation of mucoadhesive microspheres of Sitagliptin. International Journal of Pharmacy and Pharmaceutical Sciences, 5(3), 223–227.
SreeHarsha, N., Al-Dhubiab, B. E., Attimarad, M., & Nair, A. B. (2019). Preparation and evaluation of mucoadhesive Sitagliptin nanoparticles using albumin polymer. Applied Sciences, 9(1), 161. https://doi.org/10.3390/app9010161
Jana, S., Jena, B., Mohapatra, R., & Panda, P. K. (2022). Design and evaluation of microspheres containing Sitagliptin for sustained drug delivery. Journal of Pharmaceutical and Chemical Sciences, 11(3), 123–130.
Devarajan, P. V., & Sonavane, G. S. (2007). Preparation and in vitro/in vivo evaluation of gliclazide-loaded Eudragit nanoparticles as a sustained release carrier. Drug Development and Industrial Pharmacy, 33(9), 1011–1019. https://doi.org/10.1080/03639040701377882
Dora, C. P., Kushwah, V., & Jain, S. (2010). Formulation and evaluation of glibenclamide-loaded solid lipid nanoparticles for oral delivery. Journal of Drug Targeting, 18(3), 213–220. https://doi.org/10.3109/10611860903190202
Sharma, D., Maheshwari, D., Philip, G., Rana, R., Bhatia, S., & Singh, M. (2020). Formulation optimization and evaluation of nanomicelles of DPP-4 inhibitor for oral delivery. Journal of Drug Delivery Science and Technology, 57, 101627. https://doi.org/10.1016/j.jddst.2020.101627
Ding, S., Anton, N., Akram, S., & Vandamme, T. F. (2019). Preparation of double emulsions by two-step emulsification: Factors influencing the stability and application in controlled drug delivery. Advanced Drug Delivery Reviews, 147, 111–123. https://doi.org/10.1016/j.addr.2019.03.001
Gholamipour-Shirazi, A., Maleki, H., & Hamidi, M. (2008). Insulin nanoparticles using polymer-based carriers: A comprehensive review on preparation, stability, and delivery. Current Drug Delivery, 5(3), 299–306.
Prajapati, S. T., Patel, L. D., & Patel, D. M. (2008). Formulation and evaluation of microspheres of Sitagliptin phosphate for sustained release. International Journal of Pharmaceutical Sciences Review and Research, 1(2), 112–117.
Sultana, N., Arayne, M. S., & Ali, S. N. (2010). Chitosan-based delivery systems for oral sustained delivery of antidiabetic drugs. Pakistan Journal of Pharmaceutical Sciences, 23(2), 123–130.
Gupta, P., & Verma, R. K. (2012). Development and evaluation of polymeric microspheres for oral delivery of Sitagliptin. International Journal of Drug Development and Research, 4(3), 230–237
Downloads
Published
How to Cite
Issue
Section
License
This work is licensed under a Creative Commons Attribution 4.0 International License.
You are free to:
- Share — copy and redistribute the material in any medium or format
- Adapt — remix, transform, and build upon the material for any purpose, even commercially.
Terms:
- Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
- No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.
