Evaluation of bioadhesive potential and intestinal transport of pegylated poly(anhydride) nanoparticles.
Nanoparticles based on the poly(methyl vinyl ether-co-maleic anhydride) were pegylated with different types of PEGs, namely, two hydroxyl-functionalized PEGs (PEG and mPEG) and two amino-PEGs (DAE-PEG and DAP-PEG). The resulted nanoparticles demonstrated reduction of the negative surface charge compared to the non-modified particles. Further, in vivo experiments showed that all types of pegylated particles possessed higher affinity to adhere to intestinal rather than to the stomach mucosa. Higher bioadhesive potential was observed in the case of PEG-NP and DAE-PEG-NP which was attributed to the flexibility and specific properties of the surface "brush" layer of these particles. The lower bioadhesive potential of mPEG-NP was due to the low presence of coating "brush" layer, whereas for DAP-PEG-NP to the fact that the double end coupled chains ("loop"-conformation) were not available for intensive interactions with the mucosa. The observations made by optic microscopy illustrated an intracellular transport of PEG-NP in vivo with preferable location in the apical area of enterocytes.
Yoncheva
K
K
Centro Galénico, University of Navarra, Apartado 177, 31080 Pamplona, Spain.
Guembe
L
L
Campanero
M A
MA
Irache
J M
JM
D000268:Adhesiveness; D000284:Administration, Oral; D000818:Animals; D001692:Biological Transport; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers; D016503:Drug Delivery Systems; D020895:Enterocytes / Q000378:metabolism; D005753:Gastric Mucosa / Q000166:cytology / Q000378:metabolism; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000166:cytology / Q000378:metabolism; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D049388:Polyanhydrides / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D011108:Polymers / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013499:Surface Properties
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D049388:Polyanhydrides; D011108:Polymers; D011092:Polyethylene Glycols