Background: Celecoxib is a selective cyclo-oxygenase-2 inhibitor recommended orally to treat arthritis and osteoarthritis. It is a highly lipophilic, poorly soluble drug with oral bioavailability of around 40%. Long term oral administration of celecoxib causes serious gastrointestinal side effects. Objectives: The current study aimed to assess the skin permeation of celecoxib by a transdermally applied liposomal formulation. Materials and Methods: Liposomes were prepared by thin film method using soya lecithin and cholesterol. Physicochemical characteristics of the liposomes such as, particle size, drug encapsulation efficiency were determined. Also, drug release and in vitro skin permeability through rat skin were evaluated using Franz diffusion cells. Results: The results showed that the maximum drug encapsulation efficiency was 43.24%. Drug release profile showed that 81.25% of the drugs released in the first 24 hours of the experiment. Fluxes (Jss), permeability coefficient (P), diffusivity coefficient (D) parameters of the optimum liposomal formulation were significantly higher than those of saturated aqueous solution of celecoxib. The decrease of lecithin increased values. Particle sizes of the formulations ranged from 0.117 to 1.123 µm. Jss, Dapp and P parameters in L - 8 formulations were 29.18, 60.95, and 3.21 times higher than those of saturated water solution of celecoxib, respectively. The results of vesicles characterization indicated the potential application of celecoxib loaded liposome as carrier system. Conclusions: In conclusion, the components such as lecithin and cholesterol, and vortex time in liposomal formulations have an essential role in the physicochemical properties and celecoxib permeability through rat skin. Keywords: Liposome; Celecoxib; Permeability; Transdermal
20 July 2013 in Jundishapur Journal of Natural Pharmaceutical Products
Background: The increased incidence of inflammatory diseases has necessitated the need to search for new topical dosage form of dexamethasone. Objectives: The purpose of the present study was the preparation and evaluation of novel microemulsion as a topical delivery system for dexamethasone by mixing appropriate amount of surfactant including Tween 80 and Labrasol, cosurfactant such as capryol 90 and oil phase including labrafac lipophile wl-transcutol P (10:1 ratio). Materials and Methods: The prepared microemulsions were evaluated regarding their particle size, zeta potential, X-Ray scattering, conductivity, stability, viscosity, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), refractory index (RI), pH, and x-ray diffraction (XRD). Results: The results showed that the maximum oil was incorporated in microemulsion system that contained surfactant to cosurfactant ratio of 4:1. The mean droplet size range of microemulsion formulation was in the range of 5.09 to 159 nm, and its refractory index (RI) and pH were 1.44 and 7, respectively. Viscosity range was 57-226 cps. Drug release profile showed that 48.18% of the drug released in the 24 hours of experiment. Also, Hexagonal, cubic and lamellar structures were seen in the SEM photograph and XRD peak of microemulsions. Conclusions: This study demonstrated that physicochemical properties and in vitro release were dependent upon the contents of S/C, water, and oil percentage in formulations. SAXS technique and SEM obtained important information about microstructure of microemulsions. W/O and bicontinuous microemulsion with different microstructures were found in formulations. Keywords: Dexamethasone; Emulsion; Calorimetry, Differential Scanning
24 October 2019 in Advanced Pharmaceutical Bulletin
Purpose: Finasteride is a pharmaceutical agent that treats hair loss and acne with hormonalpatterns. Due to its poor water solubility, and the smaller surface area in comparison to totalskin surface area, penetration of the drug into hair follicles and skin is low. The aim of thisresearch was to formulate, characterize and evaluate in vitro skin permeability of finasteridemicroemulsions (MEs).Methods: Finasteride MEs were prepared using a pseudo-ternary phase diagram method withan appropriate ratio of oil mixture, surfactant-co-surfactant mixture and water. MEs containing1% finasteride were prepared with a suitable amount of oily phase and surfactant and cosurfactant.The physicochemical properties of these MEs and in vitro skin permeability of MEswere evaluated.Results: The results showed that the mean droplet size range of ME samples was 5–17 nm andpH was 5.1–5.7. The viscosity of MEs ranged from 86.4–209.6 cps. The drug release profileshowed that 49.510% of the drug was released (ME-F-6) over the 24 hours of the experiment.The kinetics of drug release from all selected MEs were approximately described by Higuchiand first-order modeling. All ME formulations with different compositions and propertiessignificantly increased flux and permeability coefficient from rat skin. The selected MEs exhibit99.9% finasteride after six months of storage.Conclusion: This study showed that any change in the content and composition of MEs couldchange the physical and chemical properties in addition to ME permeability parameters. TheMEs increased permeability of the skin to finasteride.
The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated. MTT cell viability assay was performed on Caco-2 cells. The well-diluted samples (200 to 1000-fold dilutions) proved to be non-cytotoxic. The acute administration of PL-SNEDDS compositions resulted in minor changes in hepatic markers (AST, ALT), except for compositions 4 and 8 due to their high Transcutol contents (80%). The non-toxic compositions showed a significant increase in free radical scavenger activity measured by the DPPH test compared to the blank SNEDDS. An indirect dissolution test was performed, based on the result of the DPPH antioxidant assay; the dissolution profiles of Plantago lancolata extract were statistically different from each SNEDDS. The anti-inflammatory effect of PL-SNEDDS compositions was confirmed by the ear inflammation test. For the complete examination period, all compositions decreased ear edema as compared to the positive (untreated) control. It can be concluded that PL-SNEDDS compositions could be used to deliver active natural compounds in a stable, efficient, and safe manner.