Formulation and Evaluation of Aciclovir Loaded Novel Gelfor Topical Application
Journal Title: Biomedical Journal of Scientific & Technical Research (BJSTR) - Year 2017, Vol 1, Issue 2
Abstract
The main objective of this work was to examine the capacity of a nano emulsion formulation for topical application of Acyclovir. Various o/w Nano emulsion were prepared by using drop by drop addition method. By constructing pseudo phase ternary diagram Nano emulsion area was identified. The optimized formulation of Nanoemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation were characterized for droplet size, polydispersity index and viscosity. Using Franz Diffusion cell and abdominal skin of rat, permeation of Acyclovir was determined. After 8 hours, Formulation NEG1 shows 90.98 % of drug permeation through the rat abdominal skin and the marketed cream shows 50.59 % of drug permeation. 50 % of the drug permeation through the skin was shows after the 3 hours which in formulation NEG1 shows the increase in permeation rat abdominal skin layers as compare the marketed cream was probably due to the mean size of internal phase droplets, which were significantly smaller in Nanoemulsions. Nanoemulsion is a novel and commercially feasible approach to improve the Topical delivery of Acyclovir and has potential to increasing the skin permeability, improving stability. Herpes simplex virus (HSV) is a double-stranded, enveloped, DNA virus. Herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) belong to the family Herpesviridae, subfamily Alpha herpesvirinae. Following initial infection, the herpes viruses become latent in the sensory neural ganglia (the trigeminal ganglion in HSV-1 infection [1] and the sacral ganglion in HSV-2 infection).ACV mainly used for the first line treatment of herpes virus infection., and varicellazoster virus (VZV).The inhibitory activity of acyclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. ACV has low oral bioavailability of 10- 20%. ACV administered by the oral, topical, & intravenous route in herpes infection [2] When administrated orally often results in general side effects, including Anaphylaxis, angioedema, fever, headache, pain, peripheral edema, gastrointestinal disturbances likes diarrhoea, nausea [3]. Topical administration of ACV (cream or ointment) has side effects like flakiness of the skin, burning or stinging feeling, or itching of skin [4]. Controlled drug delivery by topical administration produce steady-state phenomenon which is ultimately reduced systemic side effect and provide improved efficacy as compared to other dosage forms. Main disadvantage of Acyclovir is that it is poor water solubility and it is insoluble in hydrophobic solvents. So, it is not possible to produce a topical formulation which having sufficient concentration of active ingredient to produce its desired therapeutic effect and it is also difficult to optimize flux of the formulation through the skin. In case of rate of release of drug, it is also significant that any dosage form of a therapeutically active ingredient; should be stable for longer period; its potency should be retain; should not produce any colour change or produce insoluble ingredient and should also non irritating to the mucosa [5]. Materials Acyclovir was gifted from Acme Pharma, Ahmedabad, India. Capmul MCM was gifted sample from Abitec corp., USA. Sefsol 218, Sefsol228, PDD was gifted sample from Nikko chemicals, Japan. Labrafac gifted sample from Gattefosse, France. Acrysol k 150 and Acrysol el-135 gifted from Corel Pharma chem. Ltd, Ahmedabad, India. Tween 80, glycerol, PEG 400and Carbopol 934 P procured from S.D. Fine-chem. Ltd., Mumbai, India. In this project all solvents and chemical used were of analytical Reagent grade. Standard Calibration curve of Acyclovir by UV spectroscopy Standard stock solution of drug prepared by, transferring 10 mg drug in 100 ml volumetric flask, using double distilled water for dissolving and volume make up. In double distilled water Standard solution of 100μg/ml was prepared and series of 2μg, 4μg, 6μg, 8μg, 10μg, 12 μg, and 16μg concentration solutions were prepared. The absorbance of the solutions was measured by UV visible spectrophotometer at 253 nm against double distilled water as a blank and calibration curve was constructed [6].Solubility of Acyclovir: The solubility of Acyclovir in different oils (Olive Oil, Sefsol 218, Sefsol 228, PDD, Capmul MCM, and Labrafac), surfactants (Tween 80, Acrysol k 150, Acrysol EL 135, Acrysol k 380) and co-surfactants (Glycerol, PEG 400, Ethanol) was determined by Acyclovir, 100 mg was added to 2 ml of the selected co-surfactant, surfactants and oils in 2ml plastic appendrop. This mixture was mixed on the vibro-mixer on touch mode for 1-2 hours, mixture than allow to stand for 2 hours & centrifuge for 15 min. at 3000 rpm .From this centrifuge mixture supernatant was separated & 1ml sample was diluted with the 9 ml of double distilled water to yield a fine dispersion [7]. The resulting dispersion was assessed spectrophotometrically by measuring the absorbance value of the dispersion at 253 nm, using double distilled water as blank.
Authors and Affiliations
Bhupendra Prajapati, Manan Panchal, Umang Varia
Keywords
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- EP ID EP567076
- DOI 10.26717/BJSTR.2017.01.000184
- Views 226
- Downloads 0
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