Abstract
Sustained release systems for therapeutic proteins have been widely studied targeting to improve the action of these drugs. Molecular entrapping of proteins is particularly challenging due to their conformational instability. We have developed a micro-structured poly-epsilon-caprolactone (PCL) particle system loaded with human insulin using a simple double-emulsion w/o/w method followed by solvent evaporation method. This formulation is comprised by spheric-shaped microparticles with average size of 10 micrometers. In vitro release showed a biphasic behavior such as a rapid release with about 50% of drug delivered within 2 hours and a sustained phase for up to 48 h. The subcutaneous administration of microencapsulated insulin showed a biphasic effect on glycemia in streptozotocin-induced diabetic mice, compatible with short and intermediate-acting behaviors, with first transition peak at about 2 h and the second phase exerting effect for up to 48h after s.c. administration. This study reveals that a simplified double-emulsion system results in biocompatible human-insulin-loaded PCL microparticles that might be used for further development of optimized sustained release formulations of insulin to be used in the restoration of hormonal levels.
Highlights
The World Health Organization (WHO) estimates that more than 180 million people worldwide are diabetic and this health problem is responsible for 5% of all deaths each year (Wild et al, 2004; Roglic et al, 2005)
The developments of pharmaceutical compositions, which reduce the number of insulin shots, are needed for both better glycemic control and for improving patient’s quality of life
We report here a simple method based on double emulsification followed by simple vacuum solvent extraction for the production of PCL microparticles comprising bioactive insulin
Summary
The World Health Organization (WHO) estimates that more than 180 million people worldwide are diabetic and this health problem is responsible for 5% of all deaths each year (Wild et al, 2004; Roglic et al, 2005). The Diabetes Mellitus (DM) is a group of chronic diseases which occur when pancreas does not produce enough insulin or there is a resistance to this hormone, and in some cases are observed production and action of insulin deficient condition increasing blood sugar level and risk of microvascular damage This hormone is composed of two chains linked by disulfide bonds, chain A with 21 amino acids and chain B with 30 amino acids. A perfect glycemic control is still a difficult task despite the number of insulin formulations in market with different pharmacokinetics characteristics (Veiseh et al, 2015). The developments of pharmaceutical compositions, which reduce the number of insulin shots, are needed for both better glycemic control and for improving patient’s quality of life.
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