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KMID : 0369820160460010079
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Jorunal of Korean Pharmaceutical Sciences
2016 Volume.46 No. 1 p.79 ~ p.89
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Nanoemulsions loaded Carbopol® 934 based gel for intranasal delivery of neuroprotective Centella asiatica extract: in?vitro and ex?vivo permeation study
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Jaiswal Maneesh
Kumar Arun
Sharma Shivani
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Abstract
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The objective of the present study was to develop a formulation for sustained release of phytotherapeutics through nasal membrane for brain targeting (anti-Alzheimer) in order to overcome their low residence time and poor nasal permeability issues. A dual approach containing nanoemulsions within gel (NE-gels) was used to achieve the objectives utilizing biocompatible biomaterials. Nanoemulsions were characterized for particle size and zeta potential. NE-gels loaded with Centella asiatica (CA) extract were developed using Carbopol® 934 and were characterized for rheological properties (spreadability, viscosity), drug release and prolong anti-oxidant profile. In vitro nasal permeation and free radical scavenging activity were performed to investigate their expected sustained pharmacological responses. With increasing Carbopol® content, viscosity of NE-gels was found to increase up to 6237.3 ± 1.1 cp which adversely influenced the spreadability (3.06 ± 0.98) of the NE-gels. Enhancement in sustained release of the CA extract across the nasal membrane (four fold; up to 48 h) as well as retention time in nasal cavity (four fold; i.e. 48 h) were observed with NE-gels in comparison to CA solution (i.e. 12 h). In vitro nasal permeation study showed ~10 folds enhancement of percentage drug permeation across the nasal mucosa in comparison to extract solution while three folds increase in free radical scavenging activity was observed by NE-gel (i.e. 48 h) in comparison to nanoemulsion (i.e. 24 h), respectively. Extensive in vitro investigation established these nanocarriers as suitable nanoformulations for brain targeting of water insoluble phytochemicals.
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