Abstract
Conventional drug formulations are incapable of adequate delivery of proteins and peptides for therapeutic purposes. As these molecules have very short biological half-life, multiple dosing is required to achieve the desirable therapeutic effects. Microspheres are able to encapsulate proteins and peptide in the polymeric matrix while protecting them from enzymatic degradation. In this study Bovine Serum Albumin (BSA) matrix type microspheres were fabricated using Polylactide-co-glycolide (PLGA) by double emulsion solvent evaporation method. The effects of variables such as homogenizer speed, molecular weight of polymer and the effect of pH of the water phases, were investigated against factors such as drug loading, encapsulation efficiency, morphology, size, drug distribution and release profile of the microspheres. Results, suggested that an increase in homogenization speed leads to a decrease in microsphere size. The increase in homogenization speed also caused a significant effect on the release profile only when higher molecular weight of polymer had been used.. The pH change of the internal aqueous phase led to modification of surface morphology of spheres to a porous structure that significantly increased the total amount of released protein. Integrity of protein structure was intact as shown by SDS-PAGE. According to the results, it can be concluded that we achieved a reproducible method regarding controlled protein delivery for different sizes of particles.
Highlights
There are many limitations in conventional delivery of proteins and peptides for therapeutic purposes
PLGA microspheres containing Bovine Serum Albumin (BSA) were prepared by double emulsion method designed on the basis of our previous knowledge
60 mg of BSA was dissolved in 1 mL of deionised water as the internal aqueous phase (W1) that was emulsified into a solution of PLGA (0.3 g) in 5 mL of dichloromethane using homogenization at 12000 rpm for 2 min to form w/o emulsion
Summary
There are many limitations in conventional delivery of proteins and peptides for therapeutic purposes. Enzymatic degradation of proteins and absorption limitations in gastrointestinal system prevents oral use of proteins by conventional systems (Sinha, Trehan, 2003). As some of these molecules have very short biological half-life, multiple and frequent dosage is required to achieve the desirable therapeutic effects which in turn leads to an increase in the drug associated toxicity. Microspheres have the ability to encapsulate many drugs such as small molecules, nucleic acids and proteins (Kim, Pack, 2006) Due to these properties, microspheres can be used to overcome several problems associated with conventional drug formulation by reducing the number of doses required. Reducing the adverse effect of drugs and improving the patient compliance
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