Skip to main content

Advertisement

SpringerLink
Log in

Formulation and evaluation of Adapalene-loaded nanoparticulates for epidermal localization

  • Original Article
  • Published:
Drug Delivery and Translational Research Aims and scope Submit manuscript

Abstract

Adapalene (ADP), a topically administered antiacne drug, finds limitation due to poor penetration, limited localization, and associated incompatibility of photosensitization and skin irritation. To explicate an innovative and safe method for ADP administration and alleviating the associated limitations, solid lipid nanoparticles (SLN) of ADP have been fabricated and evaluated for efficacy in the present work. The SLN were prepared using pre-emulsion sonication method and incorporated into convenient topical dosage form, hydrogels. In vitro permeation studies of the hydrogels through HCS indicated gel containing ADP-SLN showed 2-fold more accumulation in skin layers as compared to conventional ADP gel. Rheological studies demonstrated ADP-SLN gel to possess pseudoplastic behavior, occlusion and hydration studies revealed permeation effectiveness of ADP-SLN gel over conventional ADP gel while primary skin irritation studies established safety of the ADP-SLN gel upon topical application. Hence, it was concluded that the studied ADP-SLN formulation with skin localizing ability may be a promising carrier for topical delivery of ADP.

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

Similar content being viewed by others

Abbreviations

ADP:

Adapalene

SLN:

Solid lipid nanoparticles

ADP-SLN:

Adapalene-loaded solid lipid nanoparticles

GMS:

Glyceryl monosterate

PXRD:

Powder X-ray diffraction

FTIR:

Fourier transform infrared

HCS:

Human cadaver skin

PS:

Particle size

PDI:

Polydispersity index

EE:

Entrapment efficiency

RSM:

Response surface methodology

TEWL:

Trans-epidermal water loss

References

  1. Irby CE, Yentzer BA, Feldman SR. A review of ADP in the treatment of acne vulgaris. Drugs. 2004;43:421–4.

    Google Scholar 

  2. Kawashima M, Harada S, Loesche C, Miyachi Y. ADP gel 0.1% is effective and safe for Japanese patients with acne vulgaris: a randomized, multicenter, investigator-blinded, controlled study. J Dermatol Sci. 2008;49:241–8.

    Article  CAS  PubMed  Google Scholar 

  3. Sato T, Akimoto N, Kitamura K, Kurihara H, Hayashi N, Ito A. ADP suppresses sebum accumulation via the inhibition of triacylglycerol biosynthesis and perilipin expression in differentiated hamster sebocytes in-vitro. J Dermatol Sci. 2013;70:204–10.

    Article  CAS  PubMed  Google Scholar 

  4. Piskin S, Uzunali E. A review of the use of adapalene for the treatment of acne vulgaris. Ther Clin Risk Manag. 2007;3:621–4.

    PubMed Central  CAS  PubMed  Google Scholar 

  5. Muller RH, Mader K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery—a review of the state of the art. Eur J Pharm Biopharm. 2000;50:161–78.

    Article  CAS  PubMed  Google Scholar 

  6. Santos MC, Mehnert W, Schaller M, Korting HC, Gysler A, Haberland A, et al. Drug targeting by solid lipid nanoparticles for dermal use. J Drug Target. 2002;10:489–95.

    Article  Google Scholar 

  7. Shah KA, Date AA, Joshi MD, Patravale VB. Solid lipid nanoparticle of tretinoin: potential in topical delivery. Int J Pharm. 2007;345:163–71.

    Article  CAS  PubMed  Google Scholar 

  8. Leyden JJ, Shalita A, Thiboutot D, Washenik K, Webster G. Topical retinoids in inflammatory acne: a retrospective, investigator-blinded, vehicle-controlled, photographic assessment. Clin Ther. 2005;27:216–24.

    Article  CAS  PubMed  Google Scholar 

  9. Jenning V, Gysler A, Schafer-Korting M, Gohla SH. Vitamin A loaded solid lipid nanoparticles for topical use: occlusive properties and drug targeting to the upper skin. Eur J Pharm Biopharm. 2003;49:211–8.

    Article  Google Scholar 

  10. Vyas SP, Khar RK. Nanoparticles. In: Vyas SP, Khar RK, editors. Targeted and controlled drug delivery-noval carrier systems. New Delhi: CBS; 2002. p. 331–8.

    Google Scholar 

  11. Wissing SA, Muller RH. The influence of solid lipid nanoparticles on skin hydration and viscoelasticity-in vivo study. Eur J Pharm Biopharm. 2003;56:67–72.

    Article  CAS  PubMed  Google Scholar 

  12. Maia CS, Mehnert W, Schafer-Korting M. Solid lipid nanoparticles as drug carriers for topical glucocorticoids. Int J Pharm. 2000;96:165–7.

    Article  Google Scholar 

  13. Muller RH, Wissing SA, Souto EB, Barbosa CM. Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery. Int J Pharm. 2004;278:71–7.

    Article  PubMed  Google Scholar 

  14. Jensen LB, Petersson K, Neilson HM. In-vitro penetration properties of solid lipid nanoparticles in intact and barrier-impaired skin. Eur J Pharm Biopharm. 2008;79:68–75.

    Article  Google Scholar 

  15. Patel NA, Patel NJ, Patel RP. Formulation and evaluation of curcumin gel for topical evaluation. Pharm Dev Technol. 2009;14:83–92.

    Article  Google Scholar 

  16. Bhalekar MR, Pokharkar V, Madgulkar A, Patil N, Patil N. Preparation and evaluation of miconazole nitrate-loaded solid lipid nanoparticles for topical delivery. AAPS Pharm Sci Technol. 2009;10(1):289–96.

    Article  CAS  Google Scholar 

  17. Bhalekar MR, Upadhaya PG, Nalawade SD, Madgulkar AR, Kshirsagar SJ. Anti-rheumatic activity of Chloroquine-SLN gel on wistar rats using complete Freund’s adjuvant (CFA) model. Ind j rheumatol. 2015 (in press).

  18. Muller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliv Rev. 2002;54:131–55.

    Article  Google Scholar 

  19. Gohla S, Mader K, Muller RH. Solid lipid nanoparticles (SLN) for controlled drug delivery—a review of the state of the art. Eur J Pharm Biopharm. 2000;50:161–77.

    Article  PubMed  Google Scholar 

  20. Solanki AB, Parikh JR, Parikh RH. Formulation and optimization of piroxicam proniosomes by 3-factor, 3-level Box-Behnken design. AAPS Pharm Sci Technol. 2007;8:1–7.

    Article  Google Scholar 

  21. Pachuau L, Mazumder B. A study on the effects of different surfactants on ethylcellulose microspheres. Int J PharmTechnol Res. 2009;1:966–71.

    CAS  Google Scholar 

  22. Gadhiri M, Vatanara A. Loading hydrophilic drug in solid lipid media as nanoparticles: statistical modeling of entrapment efficiency and particle size. Int J Pharm. 2012;424:128–37.

    Article  Google Scholar 

  23. Yuan H, Huang LF. Solid lipid nanoparticles prepared by solvent diffusion method in a nanoreactor system. Colloids Surfaces B. 2008;61:132–7.

    Article  CAS  Google Scholar 

  24. Wissing S, Muller RH. Solid lipid nanoparticles (SLN)—a novel carrier for UV-blockers, die pharmazie. 2001;56:783–786.

  25. Wissing SA, Muller RH. The influence of the crystallinity of lipid nanoparticles on their occlusive properties. Int J Pharm. 2002;242:377–9.

    Article  CAS  PubMed  Google Scholar 

  26. Muller RH, Hommoss A, Pardieke J. Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. Int J Pharm. 2009;366:170–84.

    Article  PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Dept. of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Pune-01, India

    Mangesh Bhalekar, Prashant Upadhaya & Ashwini Madgulkar

Authors
  1. Mangesh Bhalekar
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Prashant Upadhaya
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Ashwini Madgulkar
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Mangesh Bhalekar.

Ethics declarations

Conflict of interest

The authors report no declarations of interest.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Bhalekar, M., Upadhaya, P. & Madgulkar, A. Formulation and evaluation of Adapalene-loaded nanoparticulates for epidermal localization. Drug Deliv. and Transl. Res. 5, 585–595 (2015). https://doi.org/10.1007/s13346-015-0261-z

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s13346-015-0261-z

Keywords

Search

Navigation