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Arshia Shariff , P. K. Manna , K. L. K. Paranjothy , Mohammed Asad

Abstract

Andrographis paniculata, an established hepatoprotectant is widely used in many polyherbal formulations. The main problem with the drug is its bitterness, which causes gastric discomfort, loss of appetite, nausea and vomiting on regurgitation and in turn leads to patient non-compliance. The aim of the present study was to mask the bitterness of Andrographis paniculata to encourage its use as a monoherbal hepatoprotectant preparation. The extract of Andrographis paniculata (30%w/w of andrographolide) was entrapped into micropellets of calcium alginate for bitter taste masking and the so formed pellets were evaluated for hepatoprotectant activity in paracetamol induced hepatotoxicity in rats. The micropellets containing alcoholic extract of Andrographis paniculata equivalent to 22.5mg/kg body weight of the alcoholic extract of Andrographis paniculata were given orally to animals for a period of 9 days. The activity observed was compared with alcoholic extract of Andrographis paniculata. The bitterless alginate micropellets loaded with alcoholic extract of Andrographis paniculata were found to successfully inhibit the paracetamol induced hepatotoxiciy as indicated by a decrease in AST, ALT, ALP and liver weight. The effect observed was supported by histopathological studies. It was concluded that micropellets prepared by inotropic gelation of calcium alignate can be used to mask the bitterness of Andrographis paniculata without affecting its activity.

Keywords

Andrographis paniculata, Bitter Taste Masking, Ionotropic Gelation, Micropellets, Hepatoprotective, Paracetamol

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Vazir Ashfaq Ahmed ¹, H. G. Shiv Kumar ², K. L. K. Paranjothy ³, Mohd. Khaleel ⁴

Affiliations
1 Dept of pharmaceutics, MMU College of pharmacy, Ramanagram, Karnataka, IN
2 J.S.S. College of Pharmacy, Mysore, Karnataka, IN
3 AL-AMEEN College of Pharmacy, Bangalore, Karnataka, IN
4 Dept of Pharmaceutics, MMU College of Pharmacy, Ramanagram, Karnataka, IN

Abstract

The major purpose of this study was to investigate the effect of different polymers-based solutions as the in situ gelling vehicles for ophthalmic drug delivery. The rheological properties, in vitro release as well as in vivo studies by using various polymer solutions, like carbopol, pluronic and carbopol/pluronic solution, were evaluated. The optimum concentration of carbopol solution was 0.3% (w/v), pluronic solution was 13% (w/v). The mixture of 0.3% carbopol and 13% (w/v), pluronic solutions showed a significant enhancement in gel strength in the physiological condition; this gel mixture was also found to be free flowing . Both the in vitro release and in vivo pharmacological studies indicated that the carbopol/pluronic solution had the better ability to retain drug than the carbopol or pluronic solutions alone. The results demonstrated that the carbopol/pluronic mixture can be used as an in situ gelling vehicle to enhance the ocular bioavailability.

Keywords

Carbopol, Poloxamer 407(Pluronic F-127®) Diclofenac Potassium. Simulated Lacrimal Fluid.

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