Advertisement

Formulation and evaluation of gel containing nanostructured lipid carriers of tretinoin–Epi-β-CD binary complex for topical delivery

  • Bina Gidwani
  • Piyush Jaiswal
  • Amber Vyas
Original Article
  • 111 Downloads

Abstract

The objective of present research work was to formulate and evaluate topical gel containing tretinoin–cyclodextrin (CD) binary complex loaded into nanostructured lipid carriers (NLCs). Use of cyclodextrin and nanolipid carrier together in a system produced a synergistic effect by increasing the drug release and skin permeation, thus improving the overall therapeutic effect. Two different cyclodextrins i.e. β-CD and its water soluble polymeric derivative epichlorohydrin-β-cyclodextrin (EPI-β-CD) were used to obtain binary inclusion complex of drug-cyclodextrin (D-CD) systems by two different techniques (kneading and co-evaporation). The prepared solid complexes were characterized by FTIR, DSC, XRD etc. and the best system was selected for loading into nanolipid carriers. NLC comprising glyceryl mono stearate (GMS) and oleic acid were obtained by slightly modified emulsification evaporation method. Four different formulations of NLCs were suitability characterized for particle size, zeta potential, entrapment efficiency, drug loading and drug release. EPI-β-CD was found to be more effective than β-CD in enhancing solubility and dissolution properties of tretinoin. The most effective NLC formulation was incorporated into carbopol hydrogel which showed better permeation properties than that of the reference gel (0.1%).

Keywords

Tretinoin Nanostructured lipid carriers β-Cyclodextrin Epichlorohydrin-β-cyclodextrin Hydrogel Skin permeation 

Notes

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

References

  1. 1.
    Jenning, V.: Vitamin A loaded solid lipid nanoparticles for topical use: occlusive properties and drug targeting to the upper skin. Eur. J. Pharm. Biopharm. 49, 211–218 (2000)CrossRefGoogle Scholar
  2. 2.
    Souto, E.B., Wissing, S.A., Barbosa, C.M., Muller, R.H.: Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery. Int. J. Pharm. 278, 71–77 (2004)CrossRefGoogle Scholar
  3. 3.
    Kuchler, S., Herrmann, W., Panek-Minkin, G., Kramer, K.D., Bitt, R., Schafer-Korting, M.: SLN for topical application in skin diseases—characterization of drug carrier and carrier-target interactions. Int J Pharm. 390, 225–233 (2010)CrossRefGoogle Scholar
  4. 4.
    Lombardi, B.S.: Lipid nanoparticles for skin penetration enhancement—correlation to drug localization within the particle matrix as determined by fluorescence and parelectric spectroscopy. J. Control. Release 110, 151–163 (2005)CrossRefGoogle Scholar
  5. 5.
    Anadolu, R.Y., Sen, T., Tarimci, N., Birol, A., Erdem, C.: Improved efficacy and tolerability of retinoic acid in acne vulgaris: a new topical formulation with cyclodextrin complex Ψ. Eur. J. Acad. Dermatol. Venereol. 18, 416–421 (2004)CrossRefGoogle Scholar
  6. 6.
    Montassier, P., Duchene, D., Poelman, M.C.: In vitro release study of tretinoin from tretinoin/cyclodextrin derivative complexes. J. Incl. Phenom. Macrocycl. Chem. 31, 213–218 (1998)CrossRefGoogle Scholar
  7. 7.
    Challa, R., Ahuja, A., Ali, J., Khar, R.: Cyclodextrins in drug delivery: an updated review. AAPS PharmSciTech 6, 329–357 (2005)CrossRefGoogle Scholar
  8. 8.
    Marques, H.C.: Applications of cyclodextrins. Thermodynamic aspects of cyclodextrin complexes. Rev. Port. Farm. 44, 85–96 (1994)Google Scholar
  9. 9.
    Szente, L., Szejtli, J.: Highly soluble cyclodextrin derivatives: chemistry, properties, and trends in development. Adv. Drug Deliv. Rev. 36, 17–28 (1999)CrossRefGoogle Scholar
  10. 10.
    Layre, A.M., Gosselet, N.M., Renard, E., Sebille, B., Amiel, C.: Comparison of the complexation of cosmetic and pharmaceutical compounds with cyclodextrin, 2-hydroxypropyl-β-cyclodextrin and water-soluble β-cyclodextrin-co-epichlorohydrin polymers. J. Incl. Phenom. Macrocycl. Chem. 43, 311–317 (2002)CrossRefGoogle Scholar
  11. 11.
    Ascenso, A.: Complexation and full characterization of the tretinoin and dimethyl-β-cyclodextrin complex. AAPS PharmSciTech 12(2), 553–562 (2011)CrossRefGoogle Scholar
  12. 12.
    Mura, P., Bettinetti, G.P., Cirri, M.: Solid-state characterization and dissolution properties of naproxen–arginine–hydroxypropyl-β-cyclodextrin ternary system. Eur. J. Pharm. Biopharm. 59, 99–106 (2005)CrossRefGoogle Scholar
  13. 13.
    Lejiao, JDZ: Nanostructured lipid carriers for parenteral delivery of silybin: biodistribution and pharmacokinetic studies. Colloids Surf. B 80, 213–218 (2010)CrossRefGoogle Scholar
  14. 14.
    Ricci, M., Puglia, C., Bonina, F., Giovanni, D.C., Giovagnoli, S., Rossi, C.: Evaluation of indomethacin percutaneous absorption from nanostructured lipid carriers (NLC): in vitro and in vivo studies. J. Pharm. Sci. 94, 1149–1159 (2005)CrossRefGoogle Scholar
  15. 15.
    Cirri, M., Bragagni, M., Mennini, N., Mura, P.: Development of a new delivery system consisting in ‘‘drug–in cyclodextrin–in nanostructured lipid carriers’’ for ketoprofen topical delivery. Eur. J. Pharmaceut. Biopharm. 80, 46–53 (2012)CrossRefGoogle Scholar
  16. 16.
    Schafer-Korting, M., Mehnert, W., Korting, H.C.: Lipid nanoparticles for improved topical application of drugs for skin diseases. Adv. Drug Deliv. Rev. 59, 427–443 (2007)CrossRefGoogle Scholar
  17. 17.
    Piyush, J., Gidwani, B.. Vyas, A.: Nanostructured lipid carriers and their current application in targeted drug delivery. Artif. Cell Nanomed. Biotech. 44(1), 27–40 (2014)Google Scholar
  18. 18.
    Gidwani, B., Vyas, A.: Synthesis, characterization and application of epichlorohydrin-β-cyclodextrin polymer. Colloid Surf. B 114, 130–137 (2014)CrossRefGoogle Scholar
  19. 19.
    Gidwani, B., Vyas, A.: Designing and evaluation of extended release matrix tablet containing altretamine–HP-β-CD inclusion complex. J. Incl. Phenom. Macrocycl. Chem. 83, 401–409 (2015)CrossRefGoogle Scholar
  20. 20.
    Gidwani, B., Vyas, A.: Inclusion complexes of bendamustine with β-CD, HP-β-CD and Epi-β-CD: in vitro and in vivo evaluation. Drug Dev. Ind. Pharm. 41(12), 1978–1988CrossRefGoogle Scholar
  21. 21.
    Gidwani, B., Vyas, A.: Pharmacokinetic study of solid-lipid-nanoparticles of altretamine complexed epichlorohydrin- β-cyclodextrin for enhanced solubility and oral bioavailability. Int. J. Biol. Macromol. 101, 24–31 (2017)CrossRefGoogle Scholar
  22. 22.
    Rajinikanth, P.S., Chellian, J.: Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil. Int. J. Nanomedicine 11, 5067–5077 (2016)CrossRefGoogle Scholar
  23. 23.
    Lason, E., Sikora, E., Ogonowski, J.: Influence of process parameters on properties of nanostructured lipid carriers (NLC) formulation. Acta Biochim. Pol. 60, 773–777 (2013)Google Scholar

Copyright information

© Springer Science+Business Media B.V. 2017

Authors and Affiliations

  1. 1.University Institute of PharmacyPt. Ravishankar Shukla UniversityRaipurIndia

Personalised recommendations