Next generation of buccadhesive excipient: Preactivated carboxymethyl cellulose.
Int J Pharm
; 500(1-2): 120-7, 2016 Mar 16.
Article
en En
| MEDLINE
| ID: mdl-26773600
ABSTRACT
AIM:
Assessment of preactivated carboxymethyl cellulose as potential excipient for buccal drug delivery.METHODS:
Firstly, carboxymethyl cellulose (CMC) and cysteine (SH) were covalently coupled via amide bond formation to obtain thiolated carboxymethyl cellulose (CMC-SH). Further, preactivated carboxymethyl cellulose (CMC-S-S-MNA) was obtained by preactivation with 2-mercaptonicotinic acid (MNA). Sulforhodamine 101 (SRH101) was used as a model drug for permeation study through buccal mucosa. CMC-S-S-MNA was evaluated with respect to mucoadhesive and permeation enhancing effect and cytotoxicity.RESULTS:
Thiolated carboxymethyl cellulose exhibited a total amount of 112.46 ± 0.46 thiol groups. CMC-S-S-MNA exhibited around 50% of preactivated thiol groups. The preactivated polymer showed no toxic effect. Furthermore, compared to unmodified CMC, CMC-S-S-MNA revealed 3.0-fold improved mucoadhesive properties according to the rotating cylinder method and 8.8-fold enhancement in mucoadhesiveness by tensile assay, respectively.CONCLUSION:
Preactivated carboxymethyl cellulose fulfills the requirements as potential excipient of being mucoadhesive and permeation enhancing for the buccal drug delivery.Palabras clave
Texto completo:
1
Colección:
01-internacional
Asunto principal:
Portadores de Fármacos
/
Carboximetilcelulosa de Sodio
/
Cisteína
/
Excipientes
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Mucosa Bucal
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Int J Pharm
Año:
2016
Tipo del documento:
Article