FORMULATION AND CHARACTERIZATION OF CARVEDILOL NANOEMULSION ORAL LIQUID DOSAGE FORM

Authors

  • Hayder Kadhim Drais Ministry of Health, Babylon Health Directorate, Babylon, Iraq. Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq
  • Ahmed Abbas Hussein Ministry of Health, Babylon Health Directorate, Babylon, Iraq. Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq

Keywords:

Nanoemulsion, Carvedilol, Solubility studies, Peudoternary phase diagrams

Abstract

Objective: Carvedilol is antihypertensive. It is practically water insoluble. Therefore, the objective of this investigation is a formulation and characterization of carvedilol nano emulsion (NE) employing orally to increase carvedilol solubility for enhancing of carvedilol bioavailability.

Methods: The formulation components were chosen according to the solubility study. The diagrams of pseudo-ternary phase were made using the aqueous phase titration method. The formulated nanoemulsions were subjected to various thermodynamic stability assays. We selected eight of formulas that have thermodynamic stability for further optimization for various characterizations in order to select the best formula.

Results: The carvedilol NE3 considered a selected formula. It composes of 1.25 mg carvedilol per g of the nanoemulsion, 10 % of peppermint oil, 20% of tween80, 10% ethanol and 60% of distilled water. It was characterized by a low globule size range, low poly dispersity index, higher zeta potential, good pH value, efficient electroconductivity, classy percent of light transmittance, higher % drug content, acceptable low viscosity and carvedilol release was significantly higher (P<0.05) in dissolution rate. The carvedilol NE3 subject for further investigations. Fourier transformed infrared spectroscopy confirm no incompatibility between the drug and excipients. The atomic force microscopy study shows that system in nanoscale and has high stability.

Conclusion: The selected formula (carvedilol NE3) was a promising nanoemulsion formula that increases the carvedilol solubility result in an increment of its bioavailability.

 

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References

Zaheer Ahmad, Naveen Maurya, K Santosh Mishra, Imran Khan. Solubility enhancement of poorly water soluble drugs. Int J Pharm Technol 2011;3:807-23.

Chaudhar Amit y, Nagaich Upendra, Gulati Neha, Khosa VK RL. Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications. J Adv Pharm Educ Res 2012;2:32-67.

Bittner B, Mountfield RJ. Intravenous administration of poorly soluble new drug entities in early drug discovery: the potential impact of formulation on pharmacokinetics parameters. Curr Opin Drug Discovery Dev 2002;5:59–71.

Bittner B, Mountfield RJ. Formulations and related activities for the oral administration of poorly water soluble compounds in early discovery animal studies. Pharm Ind 2002;64:800–7.

Singh SK, Verma PR, Razdan B. Glibenclamide-loaded self-nano emulsifying drug delivery system: development and characterization. Drug Dev Ind Pharm 2010;36:933–45.

Fathy I Abd-Allah, Hamdy M Dawaba, Ahmed MS Ahmed. Development of a microemulsion-based formulation to improve the availability of poorly water-soluble drug. Drug Discoveries Ther 2010;4:257-66.

Srilatha R, Aparna C, Srinivas Dr Prathima, Sadanandam M. Formulation evaluation and characterization of glipizide nanoemulsion. Asian J Pharm Clin Res 2013;6:66-71.

Suresh Preeti K, Sharma Sudhanshu. Formulation and in-vitro characterization of self nano emulsifying drug delivery system of cinnarizine. Int J Comprehensive Pharm 2011;9:1-6.

Pratap Singh Bhuwanesh, Brajesh Kumar, K Jain S, Kausar Shafaat. Development and characterization of a nanoemulsion gel formulation for transdermal delivery of carvedilol. Int J Drug Dev Res 2012;4:151-61.

Fathy I Abd-Allah, Hamdy M Dawaba, Ahmed MS Ahmed. Development of a microemulsion-based formulation to improve the availability of the poorly water-soluble drug. Drug Discoveries Ther 2010;4:257-66.

S Saranya, N Chandrasekaran, Amitava Mukherjee. Antibacterial activity of eucalyptus oil nanoemulsion against Proteus mirabilis. Int J Pharm Pharm Sci 2012;4:668-71.

Sweta Tyagi, A Panda, Sagufta Khan. Formulation and evaluation of diclofenac diethylamine microemulsion incorporated in hydro gel. World J Pharm Res 2012;1:1258-319.

Chhabra Gulshan, Chuttani Krishna, Mishra Anil K, Pathak Kamla. Design and development of nanoemulsion drug delivery system of amlodipine besilate for improvement of oral bioavailability. Drug Dev Ind Pharm 2011;37:907–16.

Junyaprasert VB, Boonme P, Songkro S, Krauel K, Rades T. Transdermal delivery of hydrophobic and hydrophilic local anesthetics from O/W and W/O BRIJ 97-based microemulsions. J Pharm Pharm Sci 2007;10:288–98.

Fathy I abed-Allah, Hamdy M Dawaba, Ahmed MS Ahmed. Development of a microemulsion-based formulation to improve the availability of poorly water-soluble drug. Drug Discoveries Ther 2010;4:257-66.

Patel Rahul R, Patel Zinkal K, Patel KR, Patel MR. Formulation and evaluation of microemulsion based gel of ketoconazole. Int J Universal Pharm Biosci 2014;3:93-111.

Kumar Ankith, B Reddy, Debnath Subhashis, Babu M Niranjan. Design development and evaluation of novel anoemulsion of simvastatin. Int J Adv Pharm 2013;3:94-101.

V Darji Sweta. Formulation and in vitro evaluation of self micro emulsifying drug delivery system of carvedilol. Int J Universal Pharm BioSci 2014;3:394-405.

S Shamsheer, M Sabareesh, Khan Patan Rafi, P Sai krishna, B Sudheer. Formulation and evaluation of lisinopril dihydrate transdermal proniosomal gels. J Appl Pharm Sci 2011;1:181-5.

Dua Kamal, Pabreja Kavita, MV Ramana. Preparation, characterization and in vitro evaluation of aceclofenac solid dispersions. ARS Pharm 2010;51:57-76.

Karthikeyan S, Jeeva PA, Jerobin J, Mukherjee Amitava, Chandrasekaran N. Formulation and characterization of nanoemulsion coatings from Azadirachta indica. Int J ChemTech Res 2012;4:1566-70.

Vijaya R, Kumar S Suresh, Kamalakannan S. Preparation and in vitro evaluation of miconazole nitrate nanoemulsion using tween 20 as a surfactant for effective topical/transdermal delivery. J Chem Pharm Sci 2015;8:92-8.

Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Delivery Rev 2000;45:89–121.

Craig DQM, Barker SA, Banning D, Booth SW. An investigation into the mechanisms of self-emulsification using particle size analysis and low-frequency dielectric spectroscopy. Int J Pharm 1995;114:103–10.

Lawrencea M Jayne, Reesb Gareth D. Microemulsion-based media as novel drug delivery systems. Adv Drug Delivery Rev 2000;45:89–121.

Chanada GD, Sheth BB. Particle size reduction of emulsions by formulation design-II: effect of oil and surfactant concentration. J Pharm Sci Technol 1995;49:71-6.

Jacobs C, Kayser O, Mu¨ller RH. Nanosuspensions as a new approach for the formulation for the poorly soluble drug tarazepide. Int J Pharm 2000;196:161–4.

Hoeller S, Sperge A, Valenta C. Lecithin based nanoemulsions: a comparative study of the influence of non-ionic surfactants and the cationic phytosphingosine on physicochemical behavior and skin permeation. Int J Pharm 2009;370:181–6.

Peltola S, Saarinen-Savolainen P, Kiesvaara J, Suhonen TM, Urtti A. Microemulsions for topical delivery of estradiol. Int J Pharm 2003;254:99-107.

Prajapati Shailesh T, Dumaniya Suresh K, Patel Chhaganbhai N. Formulation and evaluation of self-nano emulsifying powder of ezetimibe. J Pharm Sci Drug Designing 2014;1:1-8.

Gopi G, Kannan K. Formulation development and optimization of nateglinide loaded ethyl cellulose nanoparticles by box-behnken design. Int J Pharm Pharm Sci 2015;7:310-5.

Sitterberg J, Özcetin A, Ehrhardt C, Bakowsky U. Utilizing atomic force microscopy for the characterization of nanoscale drug delivery systems. Eur J Pharm Biopharm 2010;74:2-13.

Published

01-12-2015

How to Cite

Drais, H. K., and A. A. Hussein. “FORMULATION AND CHARACTERIZATION OF CARVEDILOL NANOEMULSION ORAL LIQUID DOSAGE FORM”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 12, Dec. 2015, pp. 209-16, https://mail.innovareacademics.in/journals/index.php/ijpps/article/view/8949.

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Original Article(s)