Preparation and Characterization of Pitavastatin-Containing Nanoemulsions
This study focuses on the preparation, characterization, and in-vitro cytotoxicity evaluation of nanoemulsions containing pitavastatin. The aim is to enhance the intestinal absorption of pitavastatin through nanoemulsion effects, particularly the positive charge of the nanoemulsion. Various parameters, such as droplet size, size distribution, zeta potential, permeability, and formulation parameters, are investigated to optimize the nanoemulsion formulation for improved drug delivery.
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PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION, CHARACTERIZATION AND IN-VITRO CYTOTOXICITY EGE UNIVERSITY FACULTY OF PHARMACY DEPARTMENT OF PHARMACEUTICAL BIOTECHNOLOGY PHARMACEUTICA 2016 1
NANOEMULSIONS GENERAL INFORMATION disadvantages of new chemical entities advantages of nanoemulsions enhanced drug solubility poor solubility enhanced dissolution high partition coefficient enhanced drug stability high molecular weight low biotoxicity avoiding organic solvants low bioavailability scale-up nanoemulsion PHARMACEUTICA 2016 2
NANOEMULSIONS routes of application dermal/transdermal parenteral ocular oral enhanced bioavailability primaquine cefpodoxime desmopressin paclitaxel saquinavir PHARMACEUTICA 2016 3
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION, CHARACTERIZATION AND IN-VITRO CYTOTOXICITY AIM increase intestinal absorption of pitavastatin by nanoemulsion effects of the positive charge of the nanoemulsion PREPARATION Microfluidization CHARACTERIZATION droplet size size distribution zeta potential and permeability IN-VITRO CYTOTOXICITY Caco-2 cells. PHARMACEUTICA 2016 4
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION important parameters formulation parameters type and concentration of the constituents oil emulsifiers PS production parameters temperature (15 C and 25 C) pressure (300 bar and 500 bar) time (1, 2, 3, 4 and 5 minutes) PHARMACEUTICA 2016 5
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION F1 F2 oil phase % % drug oil positive charge emulsifier antioxidant water phase emulsifier preservative water ad 100 ad 100 PHARMACEUTICA 2016 6
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION F1 F2 oil phase % % pitavastatin drug oleic acid oil phytosphingosine positive charge Lipoid E 80 emulsifier alpha-tocopherol antioxidant water phase Tween 80 emulsifier potassium sorbate preservative water ad 100 ad 100 PHARMACEUTICA 2016 7
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION F1 F2 oil phase % % pitavastatin drug 0.1 0.1 oleic acid oil 20 20 phytosphingosine positive charge - 0.6 Lipoid E 80 emulsifier 1 1 alpha-tocopherol antioxidant 0.03 0.03 water phase Tween 80 emulsifier 2 2 potassium sorbate preservative 0.1 0.1 water ad 100 ad 100 PHARMACEUTICA 2016 8
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION high shear mixer microfluidization 8000 rpm, 3 min PHARMACEUTICA 2016 9
PITAVASTATIN CONTAINING NANOEMULSIONS: CHARACTERIZATION physicochemical stability physical stability droplet size size distribution zeta potential chemical stability drug content permeability and cytotoxicity PHARMACEUTICA 2016 10
PITAVASTATIN CONTAINING NANOEMULSIONS: CHARACTERIZATION F1 F1 300 0.3 1200 -50 zeta potential [mV] polydispersity index particle size [nm] 1000 -40 LD size [nm] 200 0.2 800 -30 600 -20 100 0.1 400 -10 200 0 0 0 0 1 2 3 4 5 1 2 3 4 5 time [min] time [min] particle size [nm] polydispersity index LD size [nm] zeta potential [mV] F2 F2 400 0.5 400 40 polydispersity index zeta potential [mV] particle size [nm] 0.4 300 300 30 LD size [nm] 0.3 200 200 20 0.2 100 100 10 0.1 0 0 0 0 1 2 3 4 5 1 2 3 4 5 time [min] time [min] particle size [nm] polydispersity index LD size [nm] zeta potential [mV] PHARMACEUTICA 2016 11
PITAVASTATIN CONTAINING NANOEMULSIONS: CHARACTERIZATION Permeability studies with Caco-2 cells by measuring TEER Formulations F1 F2 PT-solution Pab (cm/s) 1.49 10-6 0.0048 9.53 10-6 0.0021 8.16 10-6 0.007 Pba(cm/s) 0.81 10-7 0.0040 0.904 10-7 0.0025 1.893 10-7 0.0036 Efflux ratio 0.054 0.011 0.0095 0.002 0.023 0.003 % reduction of TEER values A B direction 13.83 0.75 27.82 1.12 24.96 0.99 Formulations F1 F2 PT solution B A direction 2.86 0.09 6.08 0.23 4.58 0.15 PHARMACEUTICA 2016 12
PITAVASTATIN CONTAINING NANOEMULSIONS: IN-VITRO CYTOTOXICITY Caco-2 100 80 cell viability % 0 h 24 h 48 h 72 h 60 40 20 0 F2 F1 PT solution PHARMACEUTICA 2016 13
PITAVASTATIN CONTAINING NANOEMULSIONS: PREPARATION, CHARACTERIZATION AND IN-VITRO CYTOTOXICITY nanoemulsions containing the poorly soluble drug pitavastatin were prepared by microfluidization the formulation F2 with PS showed the highest permeation using Caco-2 cells both nanoemulsions, with and without PS, were not cytotoxic an oral application of pitavastatin and PS containing nanoemulsions with an enhanced intestinal permeation PHARMACEUTICA 2016 14
THANK YOU FOR YOUR ATTENTION THANKS TO Dr. inel K KSAL Assis. Prof. Dr. Evren G NDO DU PHARMACEUTICA 2016 15
