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Rajesh Asija ¹, Shailendra Bhatt ¹, Sangeeta Asija ¹, Isha Shah ¹, Alpesh Yadav ¹

Affiliations
1 Maharishi Arvind Institute of Pharmacy, Mansarovar, Jaipur, 302020, IN

Abstract

Aim of the present study is to improve solubility of nebivolol by different technological approaches during the pharmaceutical product development. Solid dispersion technique using wide variety of carriers such as PEG 6000 and PVP K30 were prepared in ratio 1:1, 1:3 and 1:5 by fusion and solvent evaporation method. All the solid dispersions were evaluated for drug content, phase solubility, in vitro dissolution study. Solubility of PEG 6000 and PVP K30 indicates a linear relationship (A_L type of curve) in the investigated polymer concentration range. The Gibb's free energy showed declined trend with increase in the carrier concentrations. Different drug-carrier concentration level fitted to different kinetic model and it was found that solid dispersions exhibited fickian diffusional characteristics and best fitted to Higuchi model. A PVP K30 solid dispersion (1:5 ratio) prepared by solvent evaporation method showed faster dissolution rate (93.31 %) in 30 min among studied solid dispersions. The overall results showed that process of nebivolol transfer from water to carrier solution is more favorable at higher level of PVP K30. The solid dispersion of drug: PVP K 30 (1:5 ratio) prepared by solvent evaporation method was found to be optimum in term of solubility and dissolution rate. Hence, we can concluded that solubility of nebivolol can be enhanced using this carrier ratio.

Keywords

Nebivolol, Solid Dispersion, Fusion Method, Solvent Evaporation Method, PEG 6000, PVP K30.

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J. Patel Chirag ¹, Satyanand Tyagi ², Patel Pinkesh ¹, Alpesh Yadav ¹

Affiliations
1 Maharishi Arvind Institute of Pharmacy, Mansarovar, Jaipur, Rajasthan-302020, IN
2 Tyagi Pharmacy Association, Chattarpur, New Delhi-110074, IN

Abstract

Now a day the use of herbal medicines has been increased all over the world due to their excellent and miraculous therapeutic effects and fewer side effects as compared to the modern medicines. Most of phytoconstituents of herbal extracts are water soluble and poorly miscible with oils and other lipids. Lipid solubility and molecular size of phytoconstituents are the major limiting factors for molecule to pass the biological membrane to be absorbed systemically following the oral or topical administration. The bioavailability of phytoconstituents can be increased by use of novel drug delivery system, which can increase the phytoconstituents solubility in gastrointestinal fluid as well as capacity to cross lipid rich biological membrane. Complexation of phytoconstituents with phospholipids or phosphotidylcholine results in novel drug delivery system called Phytosomes. The term phytosomes is coined from two different terms: 'phyto' meaning plant and 'some' meaning cell like. Phytosomes are small in size and are cell like structures. The phytosome technology creates intermolecular bonding between individual polyphenol molecules and one or more molecules of the phosphatidylcholine or phospholipids. A Phytosome of herbal extract is generally more bioavailable than a simple herbal extract due to its enhanced capacity to cross the lipid-rich biomembranes. Phytosomes exhibits excellent pharmacokinetic and pharmacodynemic profile. Phytosomes can be formulated in the form of tablet, capsule, solution, suspension, emulsion, syrup. This article reviews the current trend and applications of herbal extract phytosomes as a tool of novel drug delivery system.

Keywords

Phytosomes, Phytoconstituents, Phospholipids, Bioavailability, Herbal Extracts.

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