ABSTRACT
The objective of present study was to develop hydrogel based nanoemulsion (NE) drug delivery system for transdermal delivery and evaluate its potential in in vivo anti-osteoporotic activity. NE was prepared using aqueous phase titration method and characterized for droplet size, zeta potential and morphology. It was then formulated into hydrogel based NE gel using carbopol 940 as gelling agent. NE gel was evaluated for pH, viscosity, in vitro/ex vivo permeation studies and in vivo anti-osteoporotic activity. The results indicated formation of spherical, nano sized globules of NE ranging from 11.17⯱â¯0.24 to 128.8⯱â¯0.16â¯nm with polydispersity of <0.5. In vitro and ex vivo permeation studies showed significantly higher permeation of NE as well as NE gel in comparison to fluvastatin solution indicating that NE gel can effectively penetrate through skin layers. In vivo anti-osteoporotic results demonstrated formation of new bone in trabecular region of osteoporotic rat femurs through micro-CT scanning radiographs. Biomechanical strength testing demonstrated greater load bearing capacity of rat femurs in the treated animals in comparison with the osteoporotic group. Thus, developed NE gel formulation of fluvastatin demonstrated greater potential for transdermal delivery and in the treatment of osteoporosis.
Subject(s)
Emulsions/administration & dosage , Fluvastatin/administration & dosage , Gels/administration & dosage , Osteoporosis/drug therapy , Acrylic Resins/chemistry , Administration, Cutaneous , Animals , Drug Carriers/chemistry , Drug Delivery Systems/methods , Emulsions/chemistry , Fluvastatin/chemistry , Gels/chemistry , Nanoparticles/administration & dosage , Nanoparticles/chemistry , Nanotechnology/methods , Particle Size , Rats , Skin/metabolism , Skin Absorption/drug effects , Viscosity/drug effectsABSTRACT
ABSTRACT The present work describes the development of a new high performance liquid chromatographic (HPLC) method for the determination of Cefixime trihydrate under different stress conditons as specified by ICH. For the analysis, a Phenomenex (250 x 4.6 mm, 5 µm particle size) ODS column and a SPD 20 A UV detector at 289 nm was used. The selected mobile phase was 10 mM disodium hydrogen phosphate (with 0.5% TEA, pH adjusted to 6.3 with OPA) and methanol in the ratio of 75:25 (v/v) in isocratic mode at a flow rate of 1 mL.min-1.The linear regression analysis data for the calibration plots showed good linear relationship with r2 = 0.9997 in the concentration range of 5-100 μg.mL-1. The stress degradation was performed using acid, alkali, water, hydrogen peroxide and uv light.
RESUMO O presente trabalho descreve o desenvolvimento de um novo alta performance cromatografia líquida (HPLC) método para a determinação de cefixima tri-estresse sob diferentes condições, conforme especificado pelo ICH. Para a análise, a Phenomenex (250 x 4,6 mm, 5 µm de granulometria) ODS coluna e a SPD 20 um detector de UV em 289 nm foi utilizado. A fase móvel selecionado foi de 10 mM hidrogenofosfato dissódico (com 0,5% TEA, o pH ajustado para 6,3 com OPA) e de metanol em razão de 75:25 (v/v) no modo isocrático com uma taxa de fluxo de 1 mL.min-1. A análise de regressão linear para dados da calibração parcelas apresentaram boa relação linear com r2 = 0,9997 no intervalo de concentração de cerca de 5 100 µg.mL-1. Degradação do estresse foi realizado utilizando um ácido, alcalino, a água, o peróxido de hidrogênio e luz uv.
Subject(s)
Chromatography, High Pressure Liquid/methods , Cefixime/analysis , Metabolism , /methods , Microscopy, Ultraviolet/methodsABSTRACT
The fruits of Piper cubeba have been used in Ayurvedic system of medicine for pain, tastelessness, painful urination and mouth diseases. Among its various chemical constituents, (-)-hinokinin, a trypanosomicidal dibenzylbutyrolactone lignan, is found in significant quantities. For quality evaluation of P. cubeba fruit and its commercial formulations, there is an urgent need to develop an analytical method based on (-)-hinokinin. For this purpose, an HPLC method was developed using photo diode array detector and Waters HR C18 column with gradient elution consisting of water and acetonitrile. The developed method was validated as per ICH-Q2B guidelines and found to be accurate, precise and linear over a wide range of concentrations (5-300 µg/mL). (-)-Hinokinin contents were found to be in the range of 0.005-0.109% (m/m) in various P. cubeba samples. The developed method was extended to LC-MS for further identification and characterization of (-)-hinokinin in samples. The developed method is simple, rapid and specific, and can be used as a tool for quality control of P. cubeba fruits and its commercial formulations.
ABSTRACT
The fruits of Piper cubeba have been used in Ayurvedic system of medicine for pain, tastelessness, painful urination and mouth diseases. Among its various chemical constituents, (-)-hinokinin, a trypanosomicidal dibenzylbutyrolactone lignan, is found in significant quantities. For quality evaluation of P. cubeba fruit and its commercial formulations, there is an urgent need to develop an analytical method based on (-)-hinokinin. For this purpose, an HPLC method was developed using photo diode array detector and Waters HR C18 column with gradient elution consisting of water and acetonitrile. The developed method was validated as per ICH-Q2B guidelines and found to be accurate, precise and linear over a wide range of concentrations (5–300 mg/mL). (-)-Hinokinin contents were found to be in the range of 0.005–0.109%(m/m) in various P. cubeba samples. The developed method was extended to LC–MS for further identification and characterization of (-)-hinokinin in samples. The developed method is simple, rapid and specific, and can be used as a tool for quality control of P. cubeba fruits and its commercial formulations.
