Preparation and in vitro evaluation of thienorphine-loaded PLGA nanoparticles

Autor: Yang Yang, Xiang Yang Xie, Xing Guo Mei
Rok vydání: 2014
Předmět:
Male
inorganic chemicals
0301 basic medicine
Materials science
Chemistry
Pharmaceutical
Bioadhesive
Administration
Oral
Biological Availability
Pharmaceutical Science
Nanoparticle
Nanotechnology
macromolecular substances
02 engineering and technology
Excipients
Chitosan
03 medical and health sciences
chemistry.chemical_compound
Drug Delivery Systems
Polylactic Acid-Polyglycolic Acid Copolymer
mental disorders
Animals
Humans
Distribution (pharmacology)
Lactic Acid
Surface charge
Particle Size
Rats
Wistar
Solubility
health care economics and organizations
Drug Carriers
technology
industry
and agriculture
General Medicine
Thienorphine
021001 nanoscience & nanotechnology
Buprenorphine
Rats
Bioavailability
030104 developmental biology
chemistry
Biophysics
Nanoparticles
Caco-2 Cells
0210 nano-technology
Polyglycolic Acid
Zdroj: Drug Delivery. 23:777-783
ISSN: 1521-0464
1071-7544
DOI: 10.3109/10717544.2014.916765
Popis: Poly (d,l-lactic-co-glycolide) nanoparticles (PLGA-NPs) have attracted considerable interest as new delivery vehicles for small molecules, with the potential to overcome issue such as poor drug solubility and cell permeability. However, their negative surface charge decreases bioavailability under oral administration. Recently, cationically modified PLGA-NPs has been introduced as novel carriers for oral delivery. In this study, our aim was to introduce and evaluate the physiochemical characteristics and bioadhesion of positively charged chitosan-coated PLGA-NPs (CS-PLGA-NPs), using thienorphine as a model drug. These results indicated that both CS-PLGA-NPs and PLGA-NPs had a narrow size distribution, averaging less than 130 nm. CS-PLGA-NPs was positively charged (+42.1 ± 0.4 mV), exhibiting the cationic nature of chitosan, whereas PLGA-NPs showed a negative surface charge (-2.01 ± 0.3 mV). CS-PLGA-NPs exhibited stronger bioadhesive potency than PLGA-NPs. Furthermore, the transport of thienorphine-CS-PLGA-NPs by Caco-2 cells was higher than thienorphine-PLGA-NPs or thienorphine solution. CS-PLGA-NPs were also found to significantly enhance cellular uptake compared with PLGA-NPs on Caco-2 cells. An evaluation of cytotoxicity showed no increase in toxicity in either kind of nanoparticles during the formulation process. The study proves that CS-PLGA-NPs can be used as a vector in oral drug delivery systems for thienorphine due to its positive surface charge and bioadhesive properties.
Databáze: OpenAIRE
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