Surface modification of PLGA nanoparticles by carbopol to enhance mucoadhesion and cell internalization.
Mucoadhesive poly (lactic-co-glycolic acid) (PLGA) nanoparticles having a modified shell-matrix derived from polyvinyl alcohol (PVA) and Carbopol (CP), a biodegradable polymer coating, to improve the adhesion and cell transfection properties were developed. The optimum formulations utilized a CP concentration in the range of 0.05-0.2%w/v, and were formed using modified emulsion-solvent evaporation technique. The resulting CP-PLGA nanoparticles were characterized in terms of their physical and chemical properties. The absorbed CP on the PLGA shell-matrix was found to affect the particle size and surface charge, with 0.05% CP giving rise to smooth spherical particles (0.05CP-PLGA) with the smallest size (285.90 nm), and strong negative surface charge (-25.70 mV). The introduction of CP results in an enhancement of the mucoadhesion between CP-PLGA nanoparticles and mucin particles. In vitro cell internalization studies highlighted the potential of 0.05CP-PLGA nanoparticles for transfection into SiHa cells, with uptake being time dependent. Additionally, cytotoxicity studies of CP-PLGA nanoparticles against SiHa cancer cells indicated that low concentrations of the nanoparticles were non-toxic to cells (cell viability >80%). From the various formulations studied, 0.05CP-PLGA nanoparticles proved to be the optimum model carrier having the required mucoadhesive profile and could be an alternative therapeutic efficacy carrier for targeted mucosal drug delivery systems with biodegradable polymer.
Nano Delivery System Laboratory, National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency, Pathumthani, Thailand. Electronic address: suvimol@nanotec.or.th.
Suvimol
S
Surassmo
Nano Delivery System Laboratory, National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Nattika
N
Saengkrit
Nano Delivery System Laboratory, National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Uracha Rungsardthong
UR
Ruktanonchai
Nano Delivery System Laboratory, National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Kunat
K
Suktham
Nano Delivery System Laboratory, National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Noppawan
N
Woramongkolchai
Nano Characterization Laboratory, National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Tuksadon
T
Wutikhun
Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand; Center of Excellence in Innovative Drug Delivery and Nanomedicine, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand.
Satit
S
Puttipipatkhachorn
D000180:Acrylic Resins / Q000737:chemistry*; D000269:Adhesives / Q000737:chemistry*; D002448:Cell Adhesion; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004705:Endocytosis; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D009077:Mucins / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry* / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011142:Polyvinyl Alcohol / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties
D000180:Acrylic Resins; D000269:Adhesives; D004337:Drug Carriers; D009077:Mucins; C006912:carboxypolymethylene; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011142:Polyvinyl Alcohol
Carbopol; Cell internalization; Drug delivery; Mucoadhesion; PLGA nanoparticles