Skip to main content
SpringerLink
Log in

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

  • Original Article
  • Published:
Journal of Inclusion Phenomena and Macrocyclic Chemistry Aims and scope Submit manuscript

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%).

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
Fig. 8

Similar content being viewed by others

References

  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)

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  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)

    Article  Google Scholar 

  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)

    Article  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  7. Challa, R., Ahuja, A., Ali, J., Khar, R.: Cyclodextrins in drug delivery: an updated review. AAPS PharmSciTech 6, 329–357 (2005)

    Article  Google Scholar 

  8. Marques, H.C.: Applications of cyclodextrins. Thermodynamic aspects of cyclodextrin complexes. Rev. Port. Farm. 44, 85–96 (1994)

    CAS  Google Scholar 

  9. Szente, L., Szejtli, J.: Highly soluble cyclodextrin derivatives: chemistry, properties, and trends in development. Adv. Drug Deliv. Rev. 36, 17–28 (1999)

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  11. Ascenso, A.: Complexation and full characterization of the tretinoin and dimethyl-β-cyclodextrin complex. AAPS PharmSciTech 12(2), 553–562 (2011)

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  13. Lejiao, JDZ: Nanostructured lipid carriers for parenteral delivery of silybin: biodistribution and pharmacokinetic studies. Colloids Surf. B 80, 213–218 (2010)

    Article  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  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)

    Article  Google Scholar 

  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. Gidwani, B., Vyas, A.: Synthesis, characterization and application of epichlorohydrin-β-cyclodextrin polymer. Colloid Surf. B 114, 130–137 (2014)

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  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), 1978–1988

    Article  CAS  Google Scholar 

  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)

    Article  CAS  Google Scholar 

  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)

    Article  Google Scholar 

  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 

Download references

Author information

Authors and Affiliations

  1. University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur, C.G., 492 010, India

    Bina Gidwani, Piyush Jaiswal & Amber Vyas

Authors
  1. Bina Gidwani
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Piyush Jaiswal
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Amber Vyas
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Amber Vyas.

Ethics declarations

Conflict of interest

The authors declare that they have no conflict of interest.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Gidwani, B., Jaiswal, P. & Vyas, A. Formulation and evaluation of gel containing nanostructured lipid carriers of tretinoin–Epi-β-CD binary complex for topical delivery. J Incl Phenom Macrocycl Chem 89, 315–323 (2017). https://doi.org/10.1007/s10847-017-0747-z

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10847-017-0747-z

Keywords

Search

Navigation