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Role of mucoadhesive polymers in enhancing delivery of nimodipine microemulsion to brain via intranasal route.

Pathak R, Prasad Dash R, Misra M, Nivsarkar M - Acta Pharm Sin B (2014)

Bottom Line: The purpose of this study was to evaluate the effect of mucoadhesive polymers in enhancing the delivery of nimodipine microemulsion to the brain via the intranasal route.In vitro and ex vivo permeation studies showed an initial burst of drug release at 30 min and sustained release up to 6 h, attributable to the presence of free drug entrapped in the mucoadhesive layer.These results suggest that incorporation of a mucoadhesive agent in a microemulsion intranasal delivery system can increase the retention time of the formulation and enhance brain delivery of drugs.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research-Ahmedabad, C/O - B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, Ahmedabad 380054, Gujarat, India.

ABSTRACT
Intranasal drug administration is receiving increased attention as a delivery method for bypassing the blood-brain barrier and rapidly targeting therapeutics to the CNS. However, rapid mucociliary clearance in the nasal cavity is a major hurdle. The purpose of this study was to evaluate the effect of mucoadhesive polymers in enhancing the delivery of nimodipine microemulsion to the brain via the intranasal route. The optimized mucoadhesive microemulsion was characterized, and the in vitro drug release and in vivo nasal absorption of drug from the new formulation were evaluated in rats. The optimized formulation consisted of Capmul MCM as oil, Labrasol as surfactant, and Transcutol P as co-surfactant, with a particle size of 250 nm and zeta potential value of -15 mV. In vitro and ex vivo permeation studies showed an initial burst of drug release at 30 min and sustained release up to 6 h, attributable to the presence of free drug entrapped in the mucoadhesive layer. In vivo pharmacokinetic studies in rats showed that the use of the mucoadhesive microemulsion enhanced brain and plasma concentrations of nimodipine. These results suggest that incorporation of a mucoadhesive agent in a microemulsion intranasal delivery system can increase the retention time of the formulation and enhance brain delivery of drugs.

No MeSH data available.


Pseudoternary phase diagram with varying ratios of the investigated quaternary system water/Labrasol/Transcutol/capmul MCM with (a) Smix in the ratio of 1:1 (b) Smix in the ratio of 2:1 and (c) Smix in the ratio of 3:1. The shaded areas indicate the clear o/w microemulsion system.
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f0010: Pseudoternary phase diagram with varying ratios of the investigated quaternary system water/Labrasol/Transcutol/capmul MCM with (a) Smix in the ratio of 1:1 (b) Smix in the ratio of 2:1 and (c) Smix in the ratio of 3:1. The shaded areas indicate the clear o/w microemulsion system.

Mentions: The selection of oils, surfactants and co-surfactants and the surfactant/co-surfactant ratios plays an important role in the formulation of microemulsion. The formulation of nimodipine microemulsion was optimized by evaluating the microemulsion regions using pseudoternary phase diagrams. A pseudoternary phase diagram of the investigated quaternary system water/Labrasol/Transcutol/Capmul MCM is presented in Fig. 2 and it shows phase diagrams with different S/CoS. The shaded areas indicate the clear o/w microemulsion system. The phase study revealed that the maximum proportion of oil was incorporated in the microemulsion system when the surfactant/co-surfactant ratio was 2:1.


Role of mucoadhesive polymers in enhancing delivery of nimodipine microemulsion to brain via intranasal route.

Pathak R, Prasad Dash R, Misra M, Nivsarkar M - Acta Pharm Sin B (2014)

Pseudoternary phase diagram with varying ratios of the investigated quaternary system water/Labrasol/Transcutol/capmul MCM with (a) Smix in the ratio of 1:1 (b) Smix in the ratio of 2:1 and (c) Smix in the ratio of 3:1. The shaded areas indicate the clear o/w microemulsion system.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4590727&req=5

f0010: Pseudoternary phase diagram with varying ratios of the investigated quaternary system water/Labrasol/Transcutol/capmul MCM with (a) Smix in the ratio of 1:1 (b) Smix in the ratio of 2:1 and (c) Smix in the ratio of 3:1. The shaded areas indicate the clear o/w microemulsion system.
Mentions: The selection of oils, surfactants and co-surfactants and the surfactant/co-surfactant ratios plays an important role in the formulation of microemulsion. The formulation of nimodipine microemulsion was optimized by evaluating the microemulsion regions using pseudoternary phase diagrams. A pseudoternary phase diagram of the investigated quaternary system water/Labrasol/Transcutol/Capmul MCM is presented in Fig. 2 and it shows phase diagrams with different S/CoS. The shaded areas indicate the clear o/w microemulsion system. The phase study revealed that the maximum proportion of oil was incorporated in the microemulsion system when the surfactant/co-surfactant ratio was 2:1.

Bottom Line: The purpose of this study was to evaluate the effect of mucoadhesive polymers in enhancing the delivery of nimodipine microemulsion to the brain via the intranasal route.In vitro and ex vivo permeation studies showed an initial burst of drug release at 30 min and sustained release up to 6 h, attributable to the presence of free drug entrapped in the mucoadhesive layer.These results suggest that incorporation of a mucoadhesive agent in a microemulsion intranasal delivery system can increase the retention time of the formulation and enhance brain delivery of drugs.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research-Ahmedabad, C/O - B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, Ahmedabad 380054, Gujarat, India.

ABSTRACT
Intranasal drug administration is receiving increased attention as a delivery method for bypassing the blood-brain barrier and rapidly targeting therapeutics to the CNS. However, rapid mucociliary clearance in the nasal cavity is a major hurdle. The purpose of this study was to evaluate the effect of mucoadhesive polymers in enhancing the delivery of nimodipine microemulsion to the brain via the intranasal route. The optimized mucoadhesive microemulsion was characterized, and the in vitro drug release and in vivo nasal absorption of drug from the new formulation were evaluated in rats. The optimized formulation consisted of Capmul MCM as oil, Labrasol as surfactant, and Transcutol P as co-surfactant, with a particle size of 250 nm and zeta potential value of -15 mV. In vitro and ex vivo permeation studies showed an initial burst of drug release at 30 min and sustained release up to 6 h, attributable to the presence of free drug entrapped in the mucoadhesive layer. In vivo pharmacokinetic studies in rats showed that the use of the mucoadhesive microemulsion enhanced brain and plasma concentrations of nimodipine. These results suggest that incorporation of a mucoadhesive agent in a microemulsion intranasal delivery system can increase the retention time of the formulation and enhance brain delivery of drugs.

No MeSH data available.