Novel approach for delivery of insulin loaded poly(lactide-co-glycolide) nanoparticles using a combination of stabilizers.
Insulin stability during microencapsulation and subsequent release is essential for retaining its biological activity. The successful delivery of insulin relies on the proper selection of stabilizers in addition to other parameters. Attempts were made to address the problem with a few combination of stabilizers for maintaining the integrity of insulin during formulation and delivery. Insulin loaded nanoparticles with different stabilizers such as pluronic F68, trehalose, and sodium bicarbonate were prepared by the double emulsion evaporation method using two different copolymer ratios of poly(DL-lactide-co-glycolide) (50:50 and 85:15). The presence of stabilizers in the nanoparticles resulted in an increase in the particle size but a reduction of encapsulation efficiency. Insulin release rate was comparatively higher for the batches containing stabilizers when compared with controls for both the copolymer ratios. Also the presence of stabilizers resulted in sustained release of insulin resulting in prolonged reduction of blood glucose levels in streptozotocin induced diabetic rats. From the in vitro and in vivo studies, we concluded that a combination of stabilizers results in beneficial effects without compromising the advantages of delivery systems.
Kumar
Podaralla Satheesh
PS
Department of Pharmacy, S.G.S. Institute of Technology and Sciences, Indore, India. satheesh.podaralla@sdstate.edu
Saini
Tulsi Ram
TR
Chandrasekar
Durairaj
D
Yellepeddi
Venkata Kashyap
VK
Ramakrishna
Sistla
S
Diwan
Prakash V
PV
D000818:Animals; D001682:Biological Availability; D001786:Blood Glucose / Q000378:metabolism; D003692:Delayed-Action Preparations / Q000737:chemistry; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D005260:Female; D006801:Humans; D007328:Insulin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D011098:Polyglactin 910 / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D017693:Sodium Bicarbonate / Q000737:chemistry; D013499:Surface Properties; D014199:Trehalose / Q000737:chemistry
D001786:Blood Glucose; D003692:Delayed-Action Preparations; D005079:Excipients; D007328:Insulin; D020442:Poloxamer; D011098:Polyglactin 910; D017693:Sodium Bicarbonate; D014199:Trehalose