Novel alginate gel microspheres produced by impinging aerosols for oral delivery of proteins.
Lysozyme and insulin were encapsulated in alginate gel microspheres using impinging aerosols method. High loadings of around 50% weight/dry microspheres weight were obtained with encapsulation efficiencies of at least 48%. Environmental scanning electron microscopy revealed smooth spherical hydrated microspheres (30-60 µm) in diameter. No lysozyme or insulin release was measured in simulated gastric fluid (HCl, pH 1.2, 37°C). Total insulin release occurred in simulated intestinal fluid (SIF; phosphate buffer saline, pH 7.4, 37°C) in 8 h following 2 h incubation in SGF and was found to retain 75% activity using the ARCHITECT® assay. Lysozyme was released completely in SIF in 10 h following 2 h incubation in SGF and was found to exhibit at least 80% bioactivity using the Micrococcus lysodeikticus assay. The absence of protein release in HCl and the retention of high levels of biological activity demonstrate the potential of alginate gel microspheres, for improving oral delivery of biopharmaceuticals.
Pharmacy Australia Centre of Excellence, The University of Queensland, Brisbane, QLD 4102, Australia.
Dewi Melani
DM
Hariyadi
Yiwei
Y
Wang
Sharon Chien-Yu
SC
Lin
Thor
T
Bostrom
Bhesh
B
Bhandari
Allan G A
AG
Coombes
D000284:Administration, Oral; D000336:Aerosols; D000464:Alginates / Q000737:chemistry*; D000818:Animals; D002417:Cattle; D003300:Copper / Q000737:chemistry; D016503:Drug Delivery Systems; D005750:Gastric Juice / Q000737:chemistry; D005782:Gels / Q000737:chemistry*; D006801:Humans; D006851:Hydrochloric Acid / Q000737:chemistry; D007328:Insulin / Q000008:administration & dosage; D008837:Micrococcus / Q000378:metabolism; D008855:Microscopy, Electron, Scanning / Q000379:methods; D008863:Microspheres; D009113:Muramidase / Q000008:administration & dosage / Q000737:chemistry; D011506:Proteins / Q000008:administration & dosage* / Q000737:chemistry; D013696:Temperature; D013997:Time Factors
D000336:Aerosols; D000464:Alginates; D005782:Gels; D007328:Insulin; D011506:Proteins; D003300:Copper; D009113:Muramidase; D006851:Hydrochloric Acid