title: Zirconium phosphatidylcholine-based nanocapsules as an in vivo degradable drug delivery system of MAP30, a momordica anti-HIV protein.
abstract: An essential in vivo drug delivery system of a momordica anti-HIV protein, MAP30, was developed through encapsulating in chemically synthesized matrices of zirconium egg- and soy-phosphatidylcholines, abbreviated to Zr/EPC and Zr/SPC, respectively. Matrices were characterized by transmission electron microscopy and powder X-ray diffractometry studies. Zr/EPC granule at an approximate diameter of 69.43±7.78 nm was a less efficient encapsulator than the granule of Zr/SPC. Interlayer spacing of the matrices encapsulating MAP30 increased from 8.8 and 9.7 Å to 7.4 and 7.9 nm, respectively. In vivo kinetics on degradation and protein release was performed by analyzing the serum sampling of intravenously injected SPF chickens. The first order and biphasic variations were obtained for in vivo kinetics using equilibrium dialysis. Antimicrobial and anti-HIV assays yielded greatly decreased MIC50 and EC50 values of nanoformulated MAP30. An acute toxicity of MAP30 encapsulated in Zr/EPC occurred at a single intravenous dose above 14.24 mg/kg bw in NIH/KM/ICR mice. The folding of MAP30 from Zr/EPC sustained in vivo chickens for more than 8 days in high performance liquid chromatography assays. These matrices could protect MAP30 efficiently with strong structure retention, lowered toxicity and prolonged in vivo life.
authors: Department of Bioscience, Luliang University, Shanxi 033001, PR China.
authors: Guo
authors: G
authors: Caizhen
authors: School of Pharmaceutical Sciences, Shanxi Medical University, Shanxi 030001, PR China.
authors: Gao
authors: G
authors: Yan
authors: School of Pharmaceutical Sciences, Shanxi Medical University, Shanxi 030001, PR China.
authors: Chang
authors: C
authors: Ronron
authors: Department of Chemical and Biological Engineering, Zhejiang University, Zhejiang 310027, PR China.
authors: Yang
authors: Y
authors: Lirong
authors: Department of Bioscience, Luliang University, Shanxi 033001, PR China.
authors: Chu
authors: C
authors: Panpan
authors: Department of Chemistry and Chemical Engineering, Luliang University, Shanxi 033001, PR China.
authors: Hu
authors: H
authors: Xuemei
authors: Graduate Institute of Pharmaceutical Chemistry, Luliang University, Shanxi 033001, PR China. Electronic address: qyb_0222@sina.com.
authors: Qiao
authors: Q
authors: Yuanbiao
authors: School of Pharmaceutical Sciences, Shanxi Medical University, Shanxi 030001, PR China. Electronic address: sxlqs2012@163.com.
authors: Li
authors: L
authors: Qingshan
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D016503:Drug Delivery Systems; D015497:HIV-1 / Q000187:drug effects*; D007275:Injections, Intravenous; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D010713:Phosphatidylcholines / Q000008:administration & dosage / Q000737:chemistry*; D054790:Ribosome Inactivating Proteins, Type 2 / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D013499:Surface Properties; D015040:Zirconium / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; C066347:MAP30 protein, Momordica charantia; D053769:Nanocapsules; D010713:Phosphatidylcholines; D054790:Ribosome Inactivating Proteins, Type 2; D015040:Zirconium
keywords: In vivo degradation and release; Nanoencapsulation; Protein structure stability; Therapeutic anti-HIV protein; Zirconium phosphatidylcholine