Analysis of the compositions of topical sprays containing nonsteroidal anti-inflammatory drugs

DOI: https://doi.org/10.29296/25419218-2020-02-02
Issue: 
2
Year: 
2020

O.A. Sushinskaya, N.S. Golyak Belarusian State Medical University, 83, Dzerzhinsky Prospect, Minsk 220116, Republic of Belarus

Nonsteroidal anti-inflammatory drugs (NSAIDs) are used to treat a number of diseases, including musculoskeletal ones. Long-term use of oral NSAIDs is associated with a high risk of adverse effects. The application of topical dosage forms, including sprays, enables these risks to be avoided. To select excipients that can achieve the optimal release of active ingredients and reduce undesirable local reactions remains relevant. Sprays are a convenient topical and local formulation that has many advantages. Pharmaceutical marketing researches revealed an insufficient number of NSAID-containing sprays in the Russian Federation, the Republic of Belarus, and Ukraine and their large number in European countries. The paper analyzes the compositions of drugs in the topical NSAID-containing sprays presented on the markets of Belarus, Russia, Ukraine, and European countries. It considers the main groups of spray excipients, in particular solvents, preservatives, skin penetration enhancers, emulsifiers, and moisturizing components. Their functions, application features, used concentrations, and application prospects when designing NSAID-containing sprays are described. Attention is paid to the risk of adverse effects due to the use of these excipients. The innovative spray formulation for topical application, such as microemulsions, that are promising two-phase transdermal drug delivery systems are considered. These are able to improve the pharmacodynamic and pharmacokinetic parameters of the drug. The microemulsions based on lecithin and on polyethoxylated hydrogenated castor oil are examined.

Keywords: 
spray
nonsteroidal anti-inflammatory drugs
excipients
microemulsions

References: 
  1. Danilov A.B. Kogda predpochtitel'no primenenie topicheskoj formy diklofenaka. Vrach, 2009; 9: 48–53. [Danilov A.B. When it is preferable to use topical form of diclofenac. Vrach, 2009; 9: 48–53 (in Russian)].
  2. Gosudarstvennyj reestr LS Ukrainy. [Elektronnoe izdanie]. Rezhim dostupa: http://www.drlz.com.ua [The State Register of drugs of Ukraine. [Electronic resource]. Access mode: http://www.drlz.com.ua (in Russian)].
  3. Smirnova E.S., Sherstjuk R.A. Moldaver B.L. Analiz sostavov lekarstvennyh preparatov s diklofenakom natrija dlja mestnogo primenenija. Remedium, 2011; 10: 43–6. [Smirnova E.S., Sherstyuk R.A., Moldaver B.L. Analysis of formulations of drugs with diclofenac sodium for local use. Remedium, 2011; 10: 43–6 (in Russian)].
  4. Crovetto S.I., Moreno E., Dib A.L. et al. Bacterial toxicity testing and antibacterial activity of parabens. Toxicological&Environmental Chemistry, 2017; 99 (5–6): 858–68.
  5. Handbook of Pharmaceutical Excipients (ed. by: Raymond C. Rowe, Paul J. Sheskey, Marian E. Quinn) UK, USA. Pharmaceutical Press and American Pharmacists Association. Electronic version. 2009.
  6. Trofimova E.S., Murashova N.M., Jurtov E.V. Mikroemul'sija na osnove letsitina. Uspehi v himii i himicheskoj tehnologii, 2016; 30 (12): 12–4. [Trofimova E.S., Murashova N.M., Yurtov E.V. Lecithin Based Microemulsion. Uspekhi v khimii i khimicheskoiu tekhnologii, 2016; 30 (12): 12–4 (in Russian)].
  7. Goh C.F., Lane M.E. Formulation of diclofenac for dermal delivery. International Journal of Pharmaceutics, 2014; 473 (1–2): 607–16.
  8. Encyclopedia of Toxicology. Third Edition, 2014; 1043-4.
  9. Sintov A.C., Botner S. Transdermal drug delivery using microemulsion and aqueous systems: Influence of skin storage conditions on the in vitro permeability of diclofenac from aqueous vehicle systems. International Journal of Pharmaceutics, 2006; 311 (1–2): 55–62.
  10. Soni M.G., Taylor S.L., Greenberg, N.A., Burdock G.A. Evaluation of the health aspects of methyl paraben: a review of the published literature. Food and Chemical Toxicology, 2002; 40 (10): 1335–73.
  11. Losenkova S.O., Stepanova E.F. Vspomogatel'nye veschestva v tehnologii transdermal'nyh lekarstvennyh form. Materialy nauchno-prakticheskoj internet-konferentsii. Kursk, 2011; 105–12. [Losenkova S.O., Stepanova E.F. Excipients in the technology of transdermal dosage forms. Materialy nauchno-prakticheskoiy internet-konferentsii. Kursk. 2011; 105–12 (in Russian)]