Kashish is currently pursuing PhD in Pharmaceutics at Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University (New Delhi, India). She received her master’s degree in Quality Assurance from the Hamdard University and awarded with University Gold Medal for securing first rank. She is also awarded with INSPIRE FELLOWSHIP by Department of science and Technology (Government of India) for a period of five years. She is a registered manufacturing chemist in sections of tablet, capsule, liquid orals,external preparations, powders and repacking by the Drug office of the state of Uttar Pradesh and have previous working experience in USFDA plant in India. Her main research interests are Novel drug delivery system, health care quality improvement and quality assurance.
Context: Inhibition of T-cell activation resulting in suppression of inflammation, therefore, in the therapy of chronic inflammatory diseases such as arthritis, dermal application of Tacrolimus (TL) in combination with colloidal approaches may leads to sustained and long term therapeutic effects.
Objective: Current work entails to development and assessment of well-tolerated colloidal carrier system containing immunosuppressant drug TL for transdermal delivery to study its efficacy against arthritis.
Methods: TL-NEs of different composition from phase diagram were prepared by high sheer homogenization and a comprehensive physico-chemical characterization of the novel systems was performed using different techniques in order to get most optimum NE. Optimized NE was incorporated in to carbopol-934 gel and subjected to ex vivo skin permeation studies, droplet size analysis, zeta potential measurement, TEM examination, Rheology and stability study. Moreover, we have evaluated the in vivo anti arthritic potential of same formulation and compared it with a marketed ointment (Protopic®, 0.03%) for the first time.
Results: Developed TL-NG formulation composed of Capryol 90 (5.0% w/w), tween-20 (15.0% w/w), Transcutol HP (7.5% w/w), water (72.5%) w/w, carbopol-934 (1.0%) and found to have permeation flux (68.88 μg/cm2/h), release (1621.46 μg/24 h), small droplet size (12.72 nm) and viscosity of 1.07 Pas. The results of ZP indicated that formulation was stable and shelf life at room temperature was calculated as 1.59 years. The in-vivo investigation demonstrated direct evidence on significant reduction (41.80%) in inflammation over a period of 24 hrs.
Conclusion: On the basis of these preliminary finding, we conclude that developed TL-NG has good anti-inflammatory action and may provide promising perspective for treatment of Arthritis.
D V R N Bhikshapathi has completed his PhD from Kakatiya University in Pharmaceutical Sciences, Warangal. He is working as Professor and Head, Dept of Pharmaceutics with 18 years of teaching and research experience in Novel Drug Delivery System. He has published more than 50 papers in reputed journals and has 2 Indian Patents.
Ensuring sufficient drug solubility is a crucial problem in pharmaceutical related research. For water-insoluble drugs, various formulation approaches are employed to enhance the solubility and dissolution rate of lead compounds. The goal of this study was to prepare and characterize solid dispersions of the poorly water soluble antidiabetic agent Linagliptin with novel water soluble carriers such as Kolliphor P 407, Kolliphor P 188, Kolliwax GMS II, Kolliphor HS15 and Soluplus in proportions viz. 1:1 & 1:3 (Drug: Carrier) with SLS as surfactant (0 to 2%) to improving its aqueous solubility and rate of dissolution by solvent evaporation technique. All the formulations showed marked improvement in the solubility behavior and improved drug release. From all the formulations SD15 was found to be optimized formulation using Kolliwax GMS II as carrier based on the solubility and dissolution studies. Analysis of X-ray diffraction of SD15 showed that Linagliptin existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Scanning electron microscopy studies suggested the conversion of crystalline Linagliptin to an amorphous form. The dissolution rate of the Linagliptin solid dispersion was greatly enhanced relative to the pure drug. The results obtained showed that the aqueous solubility and rate of dissolution was significantly improved when formulated in solid dispersion as compare to pure drug.