ABSTRACT
Flavonoids are a group of low-molecular-weight polyphenolic compounds of plant origin. They exhibit a variety of biological activities such as anti-inflammatory, antioxidant, antiviral, and antitumor etc. Baicalein, is a bioactive flavone constituent of Scutellariae radix with a wide range of beneficial activities. But the poor solubility and dissolution rate limit its oral intestinal absorption and bioavailability. The aim of this study was to develop an amphiphilic phytophospholipid complex in order to enhance the delivery of poorly soluble drug (baicalein). The baicalein-phospholipid complex (Ba-PLc) was prepared and evaluated for various physico-chemical parameters like drug loading, infrared absorption (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffractometry (X-RPD), scanning electron microscopy (SEM), aqueous/ n-octanol solubility and dissolution study. In the SEM, phospholipid complex (Ba-PLc) was found fluffy and porous with rough surface morphology. FT-IR, DSC and X-RPD data confirmed the formation of phospholipid complex. The water/ n-octanol solubility of baicalein was improved significantly in the complex. Improved dissolution was shown by the phospholipid complex. The results of the study concluded that the phospholipid complex may be considered as a promising drug delivery system for improving the absorption and overall bioavailability of the baicalein molecule.
Subject(s)
Drug Delivery Systems , Flavanones/chemistry , Phospholipids/chemistry , Calorimetry, Differential Scanning , Microscopy, Electron, Scanning , Phytotherapy , Powder Diffraction , Solubility , Spectrophotometry, Infrared , X-Ray DiffractionABSTRACT
ETHNOPHARMACOLOGICAL RELEVANCE: The stem bark of Symplocos paniculata Thunb. has been used to check abortion in folk medicine in India. AIM OF THE STUDY: The present study was undertaken to isolate the phytochemicals from the plant together with the evaluation of antimicrobial, analgesic and anti-inflammatory activities of the plant extract and isolated compounds. MATERIALS AND METHODS: The plant extract was subjected to column chromatography for isolation of phytochemicals. The agar diffusion method was adopted for antimicrobial activity to determine MICs. Ethanolic extract and isolated compounds were selected for investigating their analgesic activity on acetic acid-induced writhing response in mice. The anti-inflammatory activity was performed on carrageenan-induced paw edema in rats. RESULTS: The stem bark of the plant afforded seven compounds, 4-(8-hydroxyethyl) cyclohexan-1-oic acid (1); androst-5(6)-ene 17-one 3ß-O-(ß-d-glucopyranoside) (2); 9ß,25-cyclo 3ß-O-(ß-D glucopyranosyl)-echynocystic acid (3); 9ß,19-cyclo 24-methylcholan-5,22-diene 3ß-O-{ß-D-glucopyranosyl (1â6) α-L-rhamnopyranoside} (4); 30-ethyl 2α,16α-dihydroxy 3ß-O-(ß-D-glucopyranosyl) hopan-24-oic acid (5); 32,33,34-trimethyl-bacteriohopan-16-ene 3-O-ß-D-glucopyranoside (6) and flavone 3',4',5',6-tetramethoxy 7-O-ß-D-glucopyranosyl (1â3) ß-D-glucopyranoside (7). The extract and isolated compounds exhibited antimicrobial, analgesic and anti-inflammatory activities. CONCLUSION: The present study concludes that ethanolic extract of the plant and its constituents having significant antimicrobial, analgesic and anti-inflammatory activities.
Subject(s)
Analgesics/therapeutic use , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Magnoliopsida/chemistry , Phytotherapy , Plant Extracts/therapeutic use , Analgesics/isolation & purification , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Behavior, Animal/drug effects , Disease Models, Animal , Edema/chemically induced , Female , Inflammation/chemically induced , Inflammation/drug therapy , Male , Mice , Mice, Inbred Strains , Pain/chemically induced , Pain/drug therapy , Plant Bark , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Stems , Rats , Rats, Sprague-DawleyABSTRACT
Hair has psychological and sociological importance throughout the ages in framing the personality and general appearance of an individual. Significant progress is being made on discovering an effective and safe drug for hair growth. Angiogenesis, androgen antagonism, vasodilation, potassium channel opening and 5-alpha reductase inhibition are the major non-surgical therapeutic strategies of hair growth promotion. In spite of a flood of drugs claiming to be useful as hair growth promoters, more rational strategies, which can target the problem areas or stages of the hair growth cycle effectively, are still awaited. This article highlights the developments in hair rejuvenation strategies and reviews the potential of herbal drugs as safer and effective alternatives.
Subject(s)
Alopecia/drug therapy , Alopecia/etiology , Alopecia/physiopathology , Female , Hair/growth & development , Humans , Male , RejuvenationABSTRACT
The poor and/or erratic oral bioavailability of polyphenolics can be improved using the PHYTOSOME delivery system, a strategy that enhances the rate and the extent of solubilization into aqueous intestinal fluids and the capacity to cross biomembranes. Phospholipids show affinity for polyphenolics, and form supramolecular adducts having a definite stoichiometry. This article reviews the preparation and characterization of PHYTOSOME complexes and their activity in various medicinal (cardiovascular, anti-inflammatory, hepatoprotective, anticancer) and cosmetic (skin aging) realms of application.