Title:Development and Evaluation of PEG-gelatin-based Microparticles to Enhance
the Oral Delivery of Insulin
Volume: 30
Issue: 24
Author(s): John Alfa, Amadi Ben, Eduardo Buxaderas, Paul Akpa, Abdulmumin Hanifah, Okolo Martin-Luther Oseni, Franklin C. Kenechukwu, Momoh A. Mumuni*David Diaz Diaz*
Affiliation:
- Drug Delivery Research
Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria
- Department of Microbiology,
Faculty of Natural Sciences, Kogi State University, Ayingba, Kogi State, Nigeria
- Instituto Universitario de Bio-Orgánica Antonio González, Astrofísico
Francisco Sánchez 2, La Laguna 38206, Tenerife, Spain
- Departamento de Química Orgánica, Universidad
de La Laguna, Avda. Astrofísico Francisco Sánchez 3, La Laguna 38206, Tenerife, Spain
Keywords:
Gelatin:PEG, diabetes, toxicity, in vitro release rates, microparticles, oral delivery.
Abstract:
Background: Diabetes mellitus is a global disease identified by hyperglycemia due to defects in insulin
secretion, insulin action, or both.
Objective: The main objective of this research was to evaluate the ability of gelatinized Poly(ethylene glycol)
(PEG) microparticles to be used as carriers for oral insulin delivery via double emulsion preparation.
Methods: Five different batches of the formulation consisting of gelatin:PEG were prepared as follows: 0:1
(W1), 1:0 (W2), 1:1 (W3), 1:3 (W4), and 3:1 (W5). The prepared microparticles (from insulin-loaded batches)
had particle sizes ranging from 19.5 ± 0.32-23.9 ± 0.22 μm and encapsulation and loading capacities ranging
from 78.8 ± 0.24-88.9 ± 0.95 and 22.2 ± 0.96-29.7 ± 0.86%, respectively. The minimum and maximum in
vitro release rates were 8.0 and 66.0%, respectively, for batches W1 and W2 at 8 h.
Results: Insulin-loaded MPs induced a significant decrease in glucose levels, with a reduction from 100 to
33.35% in batch W5 at 9 h compared to that of subcutaneous insulin (100 to 22.63%). A liver function study
showed that the formulation caused no obvious toxicity to the experimental rats.
Conclusion: Gelatinized PEG-based microparticles as insulin delivery systems may open a new window into
the development of oral insulin for diabetic treatment.
