Synthesis of thiolated, PEGylated and POZylated silica nanoparticles and evaluation of their retention on rat intestinal mucosa in vitro.
Eur J Pharm Sci
; 122: 230-238, 2018 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-29969667
ABSTRACT
In this study, we synthesised thiolated silica nanoparticles using 3-mercaptopropyltrimethoxysilane and functionalised them with either 5â¯kDa methoxy polyethylene glycol maleimide (PEG) or 5â¯kDa alkyne-terminated poly(2-ethyl-2-oxazoline) (POZ). The main objectives of this study are to investigate the effects of pH on the size and ξ-potential of these nanoparticles and evaluate their mucoadhesive properties ex vivo using rat intestinal mucosa. The sizes of thiolated, PEGylated and POZylated silica nanoparticles were 53⯱â¯1, 68⯱â¯1 and 59⯱â¯1â¯nm, respectively. The size of both thiolated and POZylated nanoparticles significantly increased at pHâ¯≤â¯2, whereas no size change was observed at pHâ¯2.5-9 for both these two types of nanoparticles. On the other hand, the size of PEGylated nanoparticles did not change over the studied pH range (1.5-9). Moreover, thiolated nanoparticles were more mucoadhesive in the rat small intestine than both PEGylated and POZylated nanoparticles. After 12â¯cycles of washing (with a total of 20â¯mL of phosphate buffer solution pHâ¯6.8), a significantly greater amount of thiolated nanoparticles remained on the intestinal mucosa than FITC-dextran (non-mucoadhesive polymer, pâ¯<â¯0.005) and both PEGylated and POZylated nanoparticles (pâ¯<â¯0.05 both). However, both PEGylated and POZylated nanoparticles showed similar retention to FITC-dextran (pâ¯>â¯0.1 for both). Thus, this study indicates that thiolated nanoparticles are mucoadhesive, whereas PEGylated and POZylated nanoparticles are non-mucoadhesive in the ex vivo rat intestinal mucosa model. Each of these nanoparticles has potential applications in mucosal drug delivery.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Poliaminas
/
Polietilenoglicóis
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Silanos
/
Compostos de Sulfidrila
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Dióxido de Silício
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Nanopartículas
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Mucosa Intestinal
Limite:
Animals
Idioma:
En
Revista:
Eur J Pharm Sci
Assunto da revista:
FARMACIA
/
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Reino Unido