PLGA-lipid liposphere as a promising platform for oral delivery of proteins.
The main challenge in the oral delivery of protein drugs is to enhance their oral bioavailability. Herein, we report the uniform-sized liposphere prepared by premix membrane emulsification combined with W1/O/W2 double-emulsion method as a potential oral carrier for proteins. The protein-loaded liposphere was composed of a hydrophobic poly (D, L-lactide-co-glycolide) (PLGA) core and the lipid molecules self-assembled at the interface of W1/O and O/W2. During the preparation, the protein structure was effectively maintained. Compared with PLGA microsphere, the liposphere achieved a higher loading capacity (LC, 20.18%), entrapment efficiency (EE, 90.82%) and a lower initial burst (24.73%). Importantly, the lipospheres also showed high transcytotic efficiency with human microfold cell (M cell) model, leading to a potential enhancement of intestinal absorption. This result, together with the above studies supported that the PLGA-lipid liposphere could be a promising platform for enhancing the proteins oral bioavailability.
Department of Pharmaceutics, Shenyang Pharmaceutical University, P.O. Box 23, 103 Wenhua Road, Shenhe District, Shenyang, Liaoning 110016, PR China; National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China. Electronic address: matongtong0123@gmail.com.
Tongtong
T
Ma
National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China.
Lianyan
L
Wang
National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China.
TingyuanYang
National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China.
Dong
D
Wang
National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China. Electronic address: ghma@home.ipe.ac.cn.
Guanghui
G
Ma
Department of Pharmaceutics, Shenyang Pharmaceutical University, P.O. Box 23, 103 Wenhua Road, Shenhe District, Shenyang, Liaoning 110016, PR China. Electronic address: silingwang@syphu.edu.cn.
Siling
S
Wang
D000284:Administration, Oral; D000818:Animals; D002417:Cattle; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012710:Serum Albumin, Bovine / Q000008:administration & dosage* / Q000378:metabolism / Q000648:ultrastructure; D057900:Transcytosis
D008055:Lipids; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D012710:Serum Albumin, Bovine; D019344:Lactic Acid
Lipospheres; Oral bioavailability; Proteins; Uniform