The effect of coencapsulation of bovine insulin with cyclodextrins in ethylcellulose microcapsules.
Polymeric microcapsules have been widely investigated for protein delivery. Common problems include: low stability, low encapsulation efficiency, lack of uniformity, and burst release. Cyclodextrins (CDs) are known to enhance stability and solubility of proteins in solution. This research examines the effect of alpha-, beta-, and gamma-CDs on: (1) stability, (2) encapsulation, and (3) release of insulin from ethylcellulose microcapsules. All CDs improved thermal stability of insulin by lowering the enthalpy of unfolding by 16-52%. alpha- and gamma-CDs also increased the encapsulation efficiency of insulin and improved uniformity of the microcapsule formulations. Two mathematical models were proposed to account for insulin release and consisted of multiple zero order and first order input processes, and a single first order output process. All CDs decreased the initial burst release of insulin by up to 30%. This research demonstrates the potential for CDs to improve stability, uniformity, and encapsulation of proteins in microcapsule formulations.
Graves
R L
RL
University of the Sciences in Philadelphia, Philadelphia, Pennsylvania 19104, USA.
Makoid
M C
MC
Jonnalagadda
S
S
D000818:Animals; D002151:Calorimetry; D002214:Capsules; D002417:Cattle; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003505:Cyclodextrins / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D007004:Hypoglycemic Agents / Q000008:administration & dosage*; D007328:Insulin / Q000008:administration & dosage*; D008956:Models, Chemical; D013696:Temperature
D002214:Capsules; D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D007004:Hypoglycemic Agents; D007328:Insulin; D002482:Cellulose