Research Journal of Pharmacy and Technology

Vikram V. B. K. Mishra ¹, S. B. Bhanja ², B. B. Panigrahi ³

Affiliations
1 Department of Pharmaceutics, Research Scholar, Pacific University, Udaipur, Rajastan, IN
2 Department of Pharmaceutics, Malla Reddy college of Pharmacy (Affiliated to Osmania University), Maisammaguda, Hyderabad, Telangana State, IN
3 Hi-Tech College of Pharmacy, Bhubaneswar, Odisha, IN

Abstract

To enhance the solubility and permeability of poorly water soluble Valdecoxib, Nanoemulsion gel was formulated for the treatment of rheumatoid arthritis. Among the oils,surfactants and co-surfactants elainic acid, tween80 and ethanol were selected as they showed maximum solubility to Valdecoxib.The pseudo ternary phase-diagrams was constructed to find optimal concentration that provided the highest drug loading. The prepared Nanoemulsions were subjected trough thermodynamic stability testing.The droplet size, scanning electron microscopy (SEM) and zeta-potential were investigated.The optimized formulation of Nanoemusion NE₂ which was showing 87.63% drug release was incorporated into polymeric gel of Carbopol940 for convenient application and evaluated for viscosity, P_H, in-vitro permeations studies, skin irritation test and anti-inflammatory activity. The in-vitro skin permeations profile of optimized formulation was compared with normal Valdecoxib gel and Nanoemulsiongel NG₂.The significant increase in permeability ratio (K_p),flux (J_ss) and enhancement ratio (E_r) was observed.The anti-inflammatory effect of formulation NG₂ showed significant increase 72% inhibition effect in 24hrs when compared to Valdecoxib gel on Carrgeenan induced paw edema in rats. The results suggested that Nanoemulsion gels are potential vehicles for improved transdermal delivery of Valdecoxib.

Keywords

Nanoemulsion, Nanoemulsiongel, Scanning Electron Microscopy, in-vitro Permeations Studies, in-vivo Studies.

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R. Saisree ¹, Satyabrata Bhanja ¹, Swarup Das ¹, V. Bhavana ¹, M. Sudhakar ¹, B. B. Panigrahi ²

Affiliations
1 Department of Pharmaceutics, Mallareddy College of Pharmacy (Affiliated to Osmania University), Telangana State, IN
2 Hi-tech College of Pharmacy, Bhubaneswar, Odisha, IN

Abstract

The objective of the present study is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating mucoadhesive microspheres of valsartan. Frequent administration and variable low bioavailability (20-25%) after oral administration are problems of conventional dosage forms of valsartan. This can be attenuated by designing it in form of mucoadhesive microspheres which would prolong the residence time at the absorption site to facilitate intimate contact with absorption surface and thereby improve and enhance bioavailability.Valsartan microspheres were formulated by Emulsion Solvent Evaporation technique using polymers i.e. Xanthum Gum, Tragacanth, Carbopol 940 and HPMC K4M. All the formulations (F1-F12) were subjected to Percentage yield, Entrapment efficiency, Particle size analysis, Loose surface crystallography, Swelling index, Mucoadhesion test, In-vitro drug release studies and Scanning electron microscopy. FTIR data indicates that there was no drug interaction between drug and polymers used. Scanning electron microscopy indicated that microspheres (289±2.28μm-399±3.12μm) were spherical in shape and drug remained dispersed in polymer matrix. Among all formulations, the formulation F12 displayed better result whose Percentage yield (98.6%), Entrapment efficiency (88.9±0.17%), Swelling index (78.8±1.84mg) and In-vitro drug release was found to be 95±0.24% after 12 hours. The formulation F12 is following zero-order kinetics with non-fickian diffusion mechanism. Based on all the above evaluation parameters it was concluded that the formulation F12 was found to be the best formulation among all the formulations and can be used in the treatment of Hypertension.

Keywords

Mucoadhesive Microspheres, Entrapment Efficiency, Swelling Index, Mucoadhesion Test, In-vitro Drug Release Studies.

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