Abstract
| Language | English |
|---|---|
| Journal | International Journal of Pharmaceutics |
| Volume | 499 |
| Early online date | 30 Dec 2015 |
| DOIs | |
| Publication status | E-pub ahead of print - 30 Dec 2015 |
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Keywords
- Insulin
- PEG-PLGA
- Nanoparticles
- stability
- controlled delivery
- diabetes.
Cite this
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Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG. / haggag, Yusuf; Abdel-Wahab, Yasser; Ojo, Opeolu; Osman, Mohamed; El-Gazawy, Sanna; El-Tanani, Mohamed; Faheem, Ahmed; McCarron, Paul.
In: International Journal of Pharmaceutics, Vol. 499, 30.12.2015.Research output: Contribution to journal › Article
TY - JOUR
T1 - Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG
AU - haggag, Yusuf
AU - Abdel-Wahab, Yasser
AU - Ojo, Opeolu
AU - Osman, Mohamed
AU - El-Gazawy, Sanna
AU - El-Tanani, Mohamed
AU - Faheem, Ahmed
AU - McCarron, Paul
PY - 2015/12/30
Y1 - 2015/12/30
N2 - The aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticles (NP) prepared from poly (dl-lactic-co-glycolic acid) (PLGA) and its PEGylated diblock copolymers. Formulation parameters (type of polymer and its concentration, stabiliser concentration and volume of internal aqueous phase) and physicochemical characteristics (size, zeta potential, encapsulation efficiency, in vitro release profiles and in vitro stability) were investigated. In vivo insulin sensitivity was tested by diet-induced type II diabetic mice. Bioactivity of insulin was studied using Swiss TO mice with streptozotocin-induced type I diabetic profile. Insulin-loaded NP were spherical and negatively charged with an average diameter of 200–400 nm. Insulin encapsulation efficiency increased significantly with increasing ratio of co-polymeric PEG. The internal aqueous phase volume had a significant impact on encapsulation efficiency, initial burst release and NP size. Optimised insulin NP formulated from 10% PEG-PLGA retained insulin integrity in vitro, insulin sensitivity in vivo and induced a sustained hypoglycaemic effect from 3 hours to 6 days in type I diabetic mice.
AB - The aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticles (NP) prepared from poly (dl-lactic-co-glycolic acid) (PLGA) and its PEGylated diblock copolymers. Formulation parameters (type of polymer and its concentration, stabiliser concentration and volume of internal aqueous phase) and physicochemical characteristics (size, zeta potential, encapsulation efficiency, in vitro release profiles and in vitro stability) were investigated. In vivo insulin sensitivity was tested by diet-induced type II diabetic mice. Bioactivity of insulin was studied using Swiss TO mice with streptozotocin-induced type I diabetic profile. Insulin-loaded NP were spherical and negatively charged with an average diameter of 200–400 nm. Insulin encapsulation efficiency increased significantly with increasing ratio of co-polymeric PEG. The internal aqueous phase volume had a significant impact on encapsulation efficiency, initial burst release and NP size. Optimised insulin NP formulated from 10% PEG-PLGA retained insulin integrity in vitro, insulin sensitivity in vivo and induced a sustained hypoglycaemic effect from 3 hours to 6 days in type I diabetic mice.
KW - Insulin
KW - PEG-PLGA
KW - Nanoparticles
KW - stability
KW - controlled delivery
KW - diabetes.
U2 - 10.1016/j.ijpharm.2015.12.063
DO - 10.1016/j.ijpharm.2015.12.063
M3 - Article
VL - 499
JO - International Journal of Pharmaceutics
T2 - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
ER -