18 TH INTERNATIONAL CONFERENCE ON COMPOSITE MATERIALS IN-VITRO PERMEATION OF ANTIOXIDENT ANALOGS FOR DIABETIC VASCULAR DISEASE D.Bennet 1 , S. Kim 1 * 1 College of Bionanotechnology, Kyungwon University, Gyeonggi do, Republic of Korea * Corresponding author (samkim@kyungwon.ac.kr) Keywords : Free radical scavenger, Diabetic wound healing, Beta-carotene, Nanomaterials, Biopharmaceuticals 1 General Introduction effective strategy for reducing these problems. Oxidative stress damages lipids, protein, enzymes, Therefore, for effective approach with new strategies carbohydrate and DNA that could lead to cancer, the antioxidants should be implemented in the diabetes, cardiovascular disease and aging. treatment of diabetes [5]. Transdermal drug delivery Antioxidant neutralizes free radicals by donating one offers an alternative route for free radical scavenger of their own electrons and stopping the chain administration by the help of chemical penetration reaction. Antioxidant themselves do not become free enhancers [6]. Novel drug delivery systems (NDDS) radicals by donating an electrons because they are have an enormous impact on medical technology, stable in either form. The supposed mechanisms for significantly improving the performance of drugs in prophylaxis may include enhanced enzymatic terms of efficacy, safety and patient compliance. detoxification of harmful compounds and inhibition NDDS can greatly improve the delivery of drugs of their binding to cellular DNA [1]. Many of the which are poorly bioavailable due to their benefits derived from intake of such diets may be the unfavorable physicochemical or pharmacokinetic result of synergism between natural antioxidants and parameters. the better known vitamin antioxidants. Necessity and The presented works have utilized homogenizer to produce -Carotene nanoemulsion from biologically superiority of formulated antioxidants over dietary antioxidants is well described; however, the oral inspired biopolymer Hyaluronic acid (HA) and poly bioavailability issues remain unaddressed. The lactic acid (PLA) composite with active biomolecule dietary antioxidant bioavailability is dependent on a (Beta-carotene) by the help of emulsifier number of factors like food processing, food (Tween20) with chemical permeation enhancer deprivation, stability of the antioxidant, stabilizing ((CPE) oleic acid) . The traditional permeation effect of food matrix to restrain the release of experimental apparatus using Franz diffusion cells lipophilic antioxidants, the isomeric form present in provides a reliable in vitro technique for estimating it especially in case of carotenoids and the the permeation of drugs through the membrane. conjugated form in which it is present apart from the 2. Experimental physicochemical and biopharmaceutical properties of the active agent. The problems associated with 2.1 Preparation of nanoemulsion diabetes are a risk factor for cardiovascular disease 2.1.1. -Carotene loaded HA nanoemulsion involves nephropathy and retinopathy complications resulting cardiovascular disease leading cause of Polymeric nanoemulsion was prepared by a death in the diabetic population [2, 3]. The diabetes modified double emulsion technique [7]. Each batch control and complications needed alternative process is described as follows. At first, 30mL of treatment strategies, many researchers demonstrate double-distilled water containing Hyaluronic acid oxidative stress induced by hyperglycemia (natural, non-toxic, polysaccharide) (15mg) was generation of free radicals leads to development and emulsified with -Carotene (5mg) and 5% oleic acid progression of diabetes [4]. Excess production of (chemical penetration enhancers) containing 3mL of these free radicals results in vascular dysfunction, acetone by using a high-speed homogenization to damage to cellular proteins, membrane lipids and form primary emulsion. Next, 5mL of an aqueous nucleic acids. It clears that antioxidants might be an
phase containing tween 20 (0.194g) was UV/Vis spectrophotometer. The percentage drug immediately poured into this primary emulsion then entrapment was determined using following sonicated for 5minute by using a probe sonicator at equations. 40% amplitude then the emulsion was diluted by Mass of nanopartic le recovered adding continuous phase. Acetone was then Nanopartic le recovery (%) 100 Mass of polymeric particle, drug and evaporated off and aqueous phase concentrated by using rotary evaporation technique this evaporation excipients used in formulatio n under reduce pressure (40ºC) to final concentration Mass of drug in nanopartic le of emulsion and named as F 1-W-OA (Formulation Drug content (%, W/W) 100 Mass of nanopartic le recovered 1 with oleic acid). Mass of drug in nanopartic le 2.1.2. -Carotene loaded PLA nanoemulsion Drug entrapment (%) 100 Mass of drug used in nanopartic le formulatio n For the synthesis of -Carotene loaded PLA nanoemulsion, organic phase consist of -Carotene (5mg) and natural, non-toxic, polysaccharide PLA All the synthesis procedure was repeated three times (50mg) containing acetone (3ml) was added drop by to establish the reproducibility of nanoparticle drop in to the aqueous phase, which consist of synthesis. emulsifier tween 20 (0.194g) with 5% oleic acid and 2.4. Drug release profile emulsified with a help of high-speed homogenization to form primary emulsion. Then the In vitro release of nanomedicine formulations was procedure was followed similar to -Carotene performed by using Franz diffusion cells [9]. The donor and the receiver chambers were 1 and 5mL, loaded HA nanoemulsion and named as F 2-W-OA respectively. The receiver chamber temperature was (Formulation 2 with oleic acid). 2.2.1. Scanning electron microscopy maintained at 37±1◦C using a flow loop consisting of a water bath reservoir. The receiver chambers of The shape and surface morphology of the - the Franz diffusion cells were filled with PBS and Carotene loaded nanoparticle were examined using stirred continuously using a magnetic stir bar. Egg scanning electron microscopy (SEM). The samples shell membrane was placed between the donor and were mounted on double side adhesive carbon tapes receiver chambers with the stratum corneum facing in the metal stubs. Then the samples were coated the donor chamber. Then, 1.0mL emulsions were with platinum at 120sec under vacuum and examine placed inside the donor chambers of Franz diffusion for their morphology at 15kV. cells. At different time intervals samples were 2.3. Drug entrapment efficiency withdrawn from the receiver chamber using a syringe. Fresh PBS was replaced in the receiver The entrapment efficiency of -Carotene loaded chambers. The collected samples were stored at 4 0 C nanoemulsion was determined as described below until further analysis. The quantitative analysis [8]. Nanoparticle was separated from the medium by validated using UV/Vis spectrophotometer. And To ultracentrifugation at 15000rpm for 30 min. The investigate the mathematical mechanism of drug amount of drug present in the nanoparticle was releases from the pharmaceutical formulations were determined as the difference between the total analyzed by the following kinetic equations: zero amount of drug used to prepare the nanoemulsion order, fist order and Higuchi theoretical model [10]. and the amount of drug present in the medium. The supernatant was analyzed for drug entrapment. The 3. Results and discussion amount of drug present in the supernatant was 3.1. Development of nanoemulsion analyzed by using UV/Vis spectrophotometer. The spectrum wavelength was chosen as 450 nm for The nanoemulsions were synthesized by modified quantitative chemical analysis. The standard double emulsion technique. It was developed from calibration curve was described by developing two different natural polymers, named as F 1-W-OA different concentration of -Carotene (50–400µg) vs and F 2-W-OA. This procedure is very easy than peak area. The drug entrapment was measured using other conventional methods. -Carotene with all
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