Objective: The aim of the present study was to develop and evaluate nanostructured lipid carrier based topical hydrogel of mometasone furoate for the treatment of psoriasis. Methods: Drug loaded NLCs were successfully developed by microemulsion technique. Pseudo ternary phase diagrams were constructed using different combinations of surfactant and co-surfactants to study the microemulsion existence range. Different compositions were selected from the phase diagram showing maximum microemulsion region and were converted into NLCs by dilution in water (1:20). The optimized formulation was characterised for droplet size, zeta potential, entrapment efficiency and morphology was studied using Transmission Electron Microscopy. Ex vivo permeation studies were carried out using Wistar rat skin. The potential of this formulation in treating psoriatic inflammation was studied using imiquimod induced skin inflammation animal model. Results: The optimized formulation (F4) has droplet size of 163.2±0.522 nm, zeta potential -0.086±0.099 mV and entrapment efficiency of 60.0±0.187%. Transmission electron microscopy confirmed spherical shape of nanostructured lipid carrier. Carbopol 940 was used to convert NLC dispersion into NLC based hydrogel to improve its viscosity for topical administration. Drug permeation studies showed prolonged drug release from the NLC based gel as compared to marketed formulation following Higuchi release kinetics. The skin deposition of MF loaded NLC based hydrogel was found to 2.5 fold higher than marketed formulation with primary skin irritation index of 0.20. In vivo studies showed complete clearance of parakeratosis by treatment with the prepared NLC formulation. Accelerated stability studies signify high robustness scale of optimized formulation under one month storage period. Conclusion: The prepared NLC based formulation has proved to be a promising carrier system for the treatment of psoriasis.
30 January 2018 in Journal of Pharmaceutical Investigation
Lyotropic liquid crystalline cores are characterized as soft nanoparticles and referred as cubosomes. They are prepared to activate the natural self-assembly capability of lipids (e.g., monoolein or phytantriol) in water. Cubosomes are crystalline isotropic lipidic nanoparticles stabilized by Poloxamers such as F127, F108. It is made up of a network of two separate aqueous channels formed by a three-dimensional, non-intersecting lipid bilayer imposed over an indefinite periodic minimum surface of cubic symmetry. Cubosomes constitute unique features such as their special cubic structure which permits to incorporate highly lipophilic, hydrophilic, and amphiphilic drugs. Also, the lipids excipients used in the preparation of cubosomes such as monoolein, phytantriol are biodegradable and biocompatible so these cubic nanoparticles are referred as safe carrier for drug delivery. Cubic lipid nanoparticles have a highly stable cubic shape that allows for a slower rate of dissociation, improved drug retention, and site-specific drug delivery. The architecture of cubic particles provides suitability in the drug delivery as compared to other lipids-based drug delivery systems such as solid lipid nanoparticles (SLN), liposomes due to their drug expulsion to the surface of nanoparticles. Cubosomes with these loaded features/architectural composition led to an array of desired performance. Solvent evaporation, ultrasonication, hydrotrope, spray drying, melt dispersion emulsifying methods are used to prepare these carrier systems.
Alkannin/shikonin (A/S) and their derivatives are naturally occurring naphthoquinones majorly found in Boraginaceae family plants. They are integral constituents of traditional Chinese medicine Zicao (roots of Lithospermum erythrorhizon). In last two decades significant increase in pharmacological investigations on alkannin/shikonin and their derivatives has been reported that resulted in discovery of their novel mechanisms in various diseases and disorders. This review throws light on recently conducted pharmacological investigations on alkannin/shikonin and their derivatives and their outputs. Various analytical aspects are also discussed and brief summary of patent applications on inventions containing alkannin/shikonin and its derivatives is also provided.