Bhupen Kalita

PHYTOSOME: AN OVERVIEW

Novel drug delivery system aims to improve the shortcomings of conventional and traditional delivery systems. The novel delivery approach towards plant based drugs is gearing up and tremendous success have achieved in making phytoconstituent more bioavailable and stable. Polyphenolic phytoconstituent of flavonoid class have been known for centuries possessing diverse health giving properties but not extensively formulated to modern dosage forms due to problem in gastrointestinal absorption. A covalent complex of such phytoconstituent with phosphatidylcholine – the principle phospholipid of biological membrane makes them significantly bioavailable and stable. The complex such developed is a patented technology and given the name Phytosome. The phytosome technology markedly enhances the bioavailability of phytomedicine by making them soluble in GI fluid and enhancing lipid solubility. Important herbs including Milk thistle, Ginkgo biloba, Grape seed, Green tea, Hawthorn, Ginseng, etc. are currently available in phytosome form in the market. Phytosomal delivery is not restricted to flavonoids (polyphenol) class of phytoconstituents only, but any beneficial molecule possessing structural requirement for direct binding with phosphatidylcholine can be converted to phytosome, e.g. Andrographolide Phytosome, clarithromycin-phospholipid complex, glycerrhetinic acid-phospholipid complex, aceclophenac-phospholipid complex. Knowing the underlying objective, potentiality and diverse application of this novel phytosome technology, an attempt is accomplished to review the available literatures with research related to clinical aspect and formulation as well as success of this newer approach.

Formulation and evaluation pf Phospholipid complex of Green Tea Polyphenol

http://dx.doi.org/10.21276/IJRDPL.227 8-0238.2017.6(6).2813-2819 ABSTRACT: OBJECTIVE: Phospholipid complexes are formulated to improve absorption, bioavailability and stability of herbal product. There are many herbal extracts having excellent in-vitro activity but less in-vivo activity because of their macromolecular size and poor aqueous/lipid solubility, which result in poor absorption and bioavailability. Green tea polyphenol has poor oral bioavailability due to many known and unknown reasons and is unstable in the gastrointestinal tract. There have been published reports that encapsulating green tea polyphenols in drug delivery carrier significantly delayed its degradation in simulated digestive fluids and leads to improved oral bioavailability. METHODS: The present work aims in improving the GI dissolution and oral bioavailability of green tea extract rich in Epigallocatechin-3-gallate (EGCG) by formulating into phospholipid complex. EGCG-Phospholipid complex (EPC) was formulated by anti-solvent evaporation method using green tea extract and phosphatidylcholine (PC) in the ratio of 0.5:1, 0.75:1, 1:1, 1:0.75 and 1:0.5. RESULT: EPC were characterized by solubility, particle size, drug content, % entrapment efficacy, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and in vitro dissolution study. The results showed that the average particle size of optimized EPC formulation was 201.96 nm. The Drug content and Entrapment efficiency was found to be 90.57 ± 1.187 and 95.41 ± 0.898, respectively. In vitro drug release studies revealed that the cumulative % drug release of the optimized EPC was 98.41% at 3 hours. CONCLUSION: Results of the physicochemical and drug release studies suggested that EPC would serve as useful novel drug delivery system and provide improved oral bioavailability. ⇑ Corresponding author at: Pranjal Ray, Girijananda Chowdhury Institute of Pharmaceutical Science, Guwahati, Assam-781017, India E-mail address:pranjalray666@gmail.com

Rutin–phospholipid complex in polymer matrix for long-term delivery of rutin via skin for the treatment of inflammatory diseases

Abstract The drug with poor oral bioavailability necessitates the development of novel carrier for efficient drug delivery. This paper reports the rutin–phospholipid complex in polymer matrix for sustained delivery of rutin via the skin for the treatment of acute and chronic inflammatory diseases. Rutin in phospholipid complex (RNPs) are better soluble and permeable than the free rutin. The RNPs-loaded polymeric matrix patch with moderate adhesiveness was developed for convenient means of long term drug application on the skin. The patch was analysed for physicochemical properties, ex vivo skin permeability and in vivo efficacy in rat paw oedema model. The skin targeting efficacy was analysed by CLSM study. Optimized formulation (F2) showed 31 ± 2.32% and 26.56 ± 5.52% skin permeation at 24 h across excised rat skin and human cadaver skin, respectively. The sustained anti-inflammatory effect of the patch formulation in rat paw oedema model confirmed its unique in vivo efficacy over the conventional diclofenac gel. The CLSM study confirmed the localization of RNPs in the dermis for sustained anti-inflammatory effect. Our results suggest that the developed patch has a potential for long term site specific delivery of rutin in arthritic patients.