NDLI: The Use of Nano Polymeric Self-Assemblies Based on Novel Amphiphilic Polymers for Oral Hydrophobic Drug Delivery

Content Provider	Springer Nature Link
Author	Clare, Hoskins Lin, Paul Kong Thoo Tetley, Laurence Cheng, Woei Ping
Copyright Year	2011
Abstract	To investigate the use of nano self-assemblies formed by polyallylamine (PAA) modified with 5 or 10% mole fluorenylmethoxy carbonyl (Fmoc$_{5}$/$_{10}$), dimethylamino-1-naphthalenesulfonyl (Dansyl$_{5}$/$_{10}$) and 5% mole cholesteryl group (Ch$_{5}$) for oral hydrophobic drug delivery.Propofol, griseofulvin and prednisolone were loaded into amphiphilic PAAs. Particle size and morphology of drug-loaded self-assemblies were determined using photon correlation spectroscopy and transmission electron microscopy. Solubilising capacity, in vitro drug release and formulation stability were analysed by HPLC, and in vitro biocompatibility studies (haemolysis and cytotoxicity) were carried out on bovine erythrocytes and Caco-2 cells, respectively. Dansyl$_{10}$ and Ch$_{5}$ griseofulvin formulations were administered intra-gastrically to rats, and drug plasma levels were analysed by HPLC.Drug-encapsulated self-assemblies typically have hydrodynamic size of 300–400 nm. Dansyl$_{10}$ exhibited universal drug solubiliser property and had significantly improved prednisolone, griseofulvin and propofol solubility by 145, 557 and 224-fold, respectively. Fmoc polymers resulted in modest drug solubility improvement. These polymers were non-haemolytic, did not enhance cytotoxicity compared to unmodified PAA, and demonstrated significant increase in griseofulvin plasma concentration compared to griseofulvin in water after oral administration.Ch$_{5}$ and Dansyl$_{10}$ showed promising potential as nano-carriers for oral hydrophobic drug delivery.
Starting Page	782
Ending Page	794
Page Count	13
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	29
Issue Number	3
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2011-10-05
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Medical Law Pharmacology/Toxicology Pharmacy Biochemistry Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
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4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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