Abstract
Effective oral delivery of protein and peptide drugs remains an active topic in scientific research. In this study, matrix type microspheres were prepared with Eudragit® L100 containing N-trimethylchitosan chloride to improve the permeation of insulin across the intestinal epithelium via the paracellular pathway. Insulin loaded microspheres were initially formulated in accordance with a factorial design (23) and manufactured by means of a single water-in-oil emulsification/evaporation method. Based on external and internal morphology two microsphere formulations were selected from the initial formulations for further investigation in terms of particle size, dissolution behaviour and in vitro insulin transport across excised rat intestinal tissue. The initial eight microsphere formulations exhibited drug loading capacities ranging from 27.9–52.4% with different shapes and internal structures. The two selected microsphere formulations had average particle sizes of 157.3 ± 31.74 µm and 135.7 ± 41.05 µm, respectively, and mean dissolution time values for insulin release of 34.47 and 42.63 min, respectively. In vitro transport of insulin across excised rat intestinal tissue from the two selected microsphere formulations was 10.67–fold and 9.68–fold higher than the control group (insulin alone). The microsphere delivery system prepared from Eudragit® L100 containing N-trimethylchitosan chloride is therefore a promising candidate for effective oral insulin delivery.
Highlights
The oral route is in general the most widely and preferred route of drug administration because it improves patient compliance
Insulin as well as trimethylchitosan chloride (TMC) was successfully incorporated into microsphere formulations prepared by the emulsification solvent evaporation method
TMC was released at a faster rate than insulin from the microspheres
Summary
The oral route is in general the most widely and preferred route of drug administration because it improves patient compliance. This is due to the fact that oral administration avoids the pain and discomfort as well as the possibility of infections associated with injections. Due to advances in biotechnology, chemistry and molecular biology the production of large quantities of structurally diverse peptides and proteins is a common activity. These developments have increased the need for novel delivery systems for peptide and protein therapeutic agents [1]. To overcome the obstacles associated with oral peptide and protein drug delivery, various strategies have been suggested, such as chemical modifications including pro-drug strategies, structural modifications such as PEGylation and lipidization; targeting of transporters or tissues such as receptor-mediated endocytosis and gut associated lymphoid tissue (GALT); and formulation technologies such as particulate carriers, inclusion of absorption enhancers in dosage forms and mucoadhesive/bioadhesive systems [5]
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