Search results for: Mucoadhesive

Authors: Diky Mudhakir, M. Fauzi Bostanudin, Fiki Firmawan, Rachmat Mauludin

Abstract:

In the present study, development of salbutamol sulphate nanoparticles that adhere to gastric mucus was investigated. Salbutamol sulphate has low bioavailability due to short transit time in gastric. It also has a positive surface charge that provides hurdles to be encapsulated by the positively strong mucoadhesive polymer of chitosan. To overcome the difficulties, the surface charge of active ingredient was modified using several nonionic and anionic stomach-specific polymers. The nanoparticles were prepared using ionotropic gelation technique. The evaluation involved determination of particle size, zeta potential, entrapment efficiency, in vitro drug release and in vitro mucoadhesion test. Results exhibited that the use of anionic alginate polymer was more satisfactory than that of nonionic polymer. Characteristics of the particles was nano-size, high encapsulation efficiency, fulfilled the drug release requirements and adhesive towards stomach for around 11 hours. This result shows that the salbutamol sulphate nanoparticles can be utilized for improvement its delivery.

Keywords: Mucoadhesive, salbutamol sulphate, nanosize, anionic polymer.

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Authors: Sarunyoo Songkro, Naranut Rajatasereekul, Nipapat Cheewasrirungrueng

Abstract:

The aim of the present study was to evaluate the mucoadhesion and the release of nicotinamide gel formulations using in vitro methods. An agar plate technique was used to investigate the adhesiveness of the gels whereas a diffusion apparatus was employed to determine the release of nicotinamide from the gels. In this respect, 10% w/w nicotinamide gels containing bioadhesive polymers: Carbopol 934P (0.5-2% w/w), hydroxypropylmethyl cellulose (HPMC) (4-10% w/w), sodium carboxymethyl cellulose (SCMC) (4-6% w/w) and methylcellulose 4000 (MC) (3-5% w/w) were prepared. The gel formulations had pH values in the range of 7.14 - 8.17, which were considered appropriate to oral mucosa application. In general, the rank order of pH values appeared to be SCMC > MC4000 > HPMC > Carbopol 934P. Types and concentrations of polymers used somewhat affected the adhesiveness. It was found that anionic polymers (Carbopol 934 and SCMC) adhered more firmly to the agar plate than the neutral polymers (HPMC and MC 4000). The formulation containing 0.5% Carbopol 934P (F1) showed the highest release rate. With the exception of the formulation F1, the neutral polymers tended to give higher relate rates than the anionic polymers. For oral tissue treatment, the optimum has to be balanced between the residence time (adhesiveness) of the formulations and the release rate of the drug. The formulations containing the anionic polymers: Carbopol 934P or SCMC possessed suitable physical properties (appearance, pH and viscosity). In addition, for anionic polymer formulations, justifiable mucoadhesive properties and reasonable release rates of nicotinamide were achieved. Accordingly, these gel formulations may be applied for the treatment of oral mucosal lesions.

Keywords: Nicotinamide, bioadhesive polymer, mucoadhesiveness, release rate, gel.

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