Efficacy of nano- and microemulsion-based topical gels in delivery of ibuprofen: an in vivo study

Abstract Aim: Nanoemulsion has shown many advantages in drug delivery systems. In this study, for the first time, analgesic and anti-inflammatory properties of a nanomelusion of almond oil with and without ibuprofen was compared with corresponding microemulsion and commercial topical gel of the drug using formalin and carrageenan tests, respectively. Method: Almond oil (oil phase) was mixed with Tween 80 and Span 80 (surfactants), and ethanol (co-surfactant) and them distilled water (aqueous phase) was then added to the mixture at once. Prepared nanoemulsions were pre-emulsified into a 100 ml beaker using magnet/stirrer (1000 rpm). Then, using a probe ultrasonicator (Hielscher UP400s, Hielscher, Ringwood, NJ) the nanoemulsions were formed. Results: The optimised nanoemulsion formulation containing 2.5% ibuprofen, showed improved analgesic and anti-inflammatory effects compared with commercial product and corresponding microemulsion product containing 5% ibuprofen (i.e. twice the content of ibuprofen in the nanoemulsion) in vivo. The nanoemulsion preparation showed superior analgesic activities during chronic phase. Also, it decreased the inflammation from the first hour, while the microemulsion and the commercial product started to show their anti-inflammatory effects after 2 and 3 h, respectively. Conclusion: Our finding suggests that the size of the emulsion particles must be considered as an important factor in topical drug delivery systems.

[1]  R. Faridi‐Majidi,et al.  Anti-inflammatory effects of eugenol nanoemulsion as a topical delivery system , 2016, Pharmaceutical development and technology.

[2]  G. P. Guimarães,et al.  Microemulsion for topical application of pentoxifylline: In vitro release and in vivo evaluation. , 2016, International journal of pharmaceutics.

[3]  Jiangnan Yu,et al.  In vitro and in vivo evaluation of capsaicin-loaded microemulsion for enhanced oral bioavailability. , 2015, Journal of the science of food and agriculture.

[4]  H. El-Enshasy,et al.  Preparation, characterization and anti-inflammatory activity of swietenia macrophylla nanoemulgel , 2014 .

[5]  S. Dey,et al.  Topical delivery of aceclofenac as nanoemulsion comprising excipients having optimum emulsification capabilities: preparation, characterization and in vivo evaluation , 2013, Expert opinion on drug delivery.

[6]  A. Yavaşoğlu,et al.  Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations. , 2011, International journal of pharmaceutics.

[7]  M. Basri,et al.  Phase Behaviour, Formation and Characterization of Palm-Based Esters Nanoemulsion Formulation containing Ibuprofen , 2011 .

[8]  Wei Liu,et al.  Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability , 2011, Drug delivery.

[9]  Gregor Cevc,et al.  Nanotechnology and the transdermal route: A state of the art review and critical appraisal. , 2010, Journal of controlled release : official journal of the Controlled Release Society.

[10]  F. Shakeel,et al.  Investigation of true nanoemulsions for transdermal potential of indomethacin: characterization, rheological characteristics, and ex vivo skin permeation studies , 2009, Journal of drug targeting.

[11]  C. Valenta,et al.  Lecithin based nanoemulsions: A comparative study of the influence of non-ionic surfactants and the cationic phytosphingosine on physicochemical behaviour and skin permeation. , 2009, International journal of pharmaceutics.

[12]  Xuefeng Li,et al.  Design and optimization of a new self-nanoemulsifying drug delivery system. , 2009, Journal of colloid and interface science.

[13]  R. Nicolosi,et al.  Enhancement of anti-inflammatory property of aspirin in mice by a nano-emulsion preparation. , 2008, International immunopharmacology.

[14]  Young Yang,et al.  Antinociceptive effect of amygdalin isolated from Prunus armeniaca on formalin-induced pain in rats. , 2008, Biological & pharmaceutical bulletin.

[15]  Hun-Kuk Park,et al.  Amygdalin suppresses lipopolysaccharide-induced expressions of cyclooxygenase-2 and inducible nitric oxide synthase in mouse BV2 microglial cells , 2007, Neurological research.

[16]  Huibi Xu,et al.  Microemulsion-based hydrogel formulation of ibuprofen for topical delivery. , 2006, International journal of pharmaceutics.

[17]  P. Beaulieu,et al.  Local interactions between anandamide, an endocannabinoid, and ibuprofen, a nonsteroidal anti-inflammatory drug, in acute and inflammatory pain , 2006, Pain.

[18]  H. Raheman,et al.  Process optimization for biodiesel production from mahua (Madhuca indica) oil using response surface methodology. , 2006, Bioresource technology.

[19]  A. S. Ramadhas,et al.  Biodiesel production from high FFA rubber seed oil , 2005 .

[20]  T. Tadros,et al.  Formation and stability of nano-emulsions. , 2004, Advances in colloid and interface science.

[21]  Véronique Préat,et al.  Skin electroporation for transdermal and topical delivery. , 2004, Advanced drug delivery reviews.

[22]  J. Calixto,et al.  Efficacy, safety, quality control, marketing and regulatory guidelines for herbal medicines (phytotherapeutic agents). , 2000, Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas.

[23]  R. Melzack,et al.  The formalin test: a validation of the weighted-scores method of behavioural pain rating , 1993, Pain.

[24]  S. Hunskaar,et al.  The formalin test: an evaluation of the method , 1992, Pain.

[25]  C A WINTER,et al.  Carrageenin-Induced Edema in Hind Paw of the Rat as an Assay for Antiinflammatory Drugs , 1962, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine.