Skip to main content

Advertisement

SpringerLink
Log in

Effect of microneedles on transdermal permeation enhancement of amlodipine

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

Abstract

The present study aimed to investigate the effect of microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation enhancement of amlodipine (AMLO). Two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PM) of 0.6 mm length were employed. In the case of PMs, arrays were applied thrice at different places within a 1.77-cm2 skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Scaling analyses were done using dimensionless parameters like concentration of AMLO (Ct/Cs), thickness (h/L) and surface area of the skin (Sa/L2). Microinjection moulding technique was employed to fabricate PM. Histological studies revealed that the PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 6.84- and 6.11-fold increase in the cumulative amount (48 h) of AMLO permeated was observed with 1.5 mm ADM and PM-3 treatments respectively, when compared to passive permeation amounts. Good correlations (R 2 > 0.89) were observed between different dimensionless parameters with scaling analyses. The enhancement in AMLO permeation was found to be in the order of 1.5 mm ADM ≥ PM-3 > 1.2 mm ADM > 0.6 mm ADM ≥PM-1 > passive. The study suggests that MN application enhances the AMLO transdermal permeation and the geometrical parameters of MNs play an important role in the degree of such enhancement.

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. Brown MB, Gary PM, Stuart AJ, Franklin KA. Dermal and transdermal drug delivery systems: current and future prospects. Drug Delivery. 2006;13:175–87.

    Article  CAS  PubMed  Google Scholar 

  2. Prausnitz MR, Robert L. Transdermal drug delivery. Nat Biotechnol. 2008;26:1261–8.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  3. Nwankwo T, Yoon SS, Burt V, Gu Q. Hypertension among adults in the US: National Health and Nutrition Examination Survey, 2011–2012. NCHS Data Brief, No. 133. Hyattsville: National Center for Health Statistics, Centers for Disease Control and Prevention, US Dept of Health and Human Services; 2013.

    Google Scholar 

  4. Lim SS, Vos T, Flaxman AD, Danaei G. A comparative risk assessment of burden of disease and injury attributable to 67 risk factors and risk factor clusters in 21 regions, 1990-2010: a systematic analysis for the Global Burden of Disease Study 2010. Lancet. 2012;380(9859):2224–60.

    Article  PubMed  PubMed Central  Google Scholar 

  5. Suchanova B, Kostiainen K, Ketola RA. Characterization of the in vitro metabolic profile of amlodipine in rat using liquid chromatography–mass spectrometry. Eur J Pharm Sci. 2008;33:91–9.

    Article  CAS  PubMed  Google Scholar 

  6. Hardman JG, Limbird LE. Goodman and Gilman’s the pharmacological basis of therapeutics, vol. 10. New Delhi: McGraw Hill Medical Publishing Division; 2001. p. 853–60.

    Google Scholar 

  7. McDaid DM, Deasy PB. Formulations development of a transdermal drug delivery system for amlodipine base. Int J Pharm. 1996;133:71–83.

    Article  CAS  Google Scholar 

  8. Hemangi JP, Jitendra SP, Desai BG, Keyur DP. Permeability studies of anti-hypertensive drug amlodipine besilate for transdermal delivery. Asian Journal of Pharmaceutical and Clinical Research. 2010;3:31–4.

    Google Scholar 

  9. Sanju N, Kamal S, Bhavna Y, Benika S. Formulation and characterization of transdermal patch of amlodipine besylate. International Journal of Pharmaceutical and Chemical Sciences. 2012;1:953–69.

    Google Scholar 

  10. Lincy J, Arun K. Comparison of amlodipine transdermal patches using hydroxypropylmethylcellulose and chitosan. Asian J Pharm Clin Res. 2014;7:86–90.

    Google Scholar 

  11. Han T, Das DB. Potential of combined ultrasound and microneedles for enhanced transdermal drug permeation: a review. Eur J Pharm Biopharm. 2015;89:312–28.

    Article  CAS  PubMed  Google Scholar 

  12. Gill HS, Denson DD, Burris BA, Prausnitz MR. Effect of microneedle design on pain in human volunteers. Clin J Pain. 2008;24:585–94.

    Article  PubMed  PubMed Central  Google Scholar 

  13. Jeong W, Lee A, Jung-Hwan PB. Prausnitz MR. Dissolving microneedles for transdermal drug delivery biomaterials. 2008;29:2113–24.

    Google Scholar 

  14. Zhou CP, Liu YL, Wang HL, Zhang PX, Zhang JL. Transdermal delivery of insulin using microneedle rollers in vivo. Int J Pharm. 2010;39:127–33.

    Article  Google Scholar 

  15. Nalluri BN, Sai Sri Anusha V, Bramhini SR, Amulya J, Sultana AS, Teja UC, Das DB. In vitro skin permeation enhancement of sumatriptan by microneedle application. Curr Drug Deliv 2015;12:761–769.

  16. Monika K, Kevin BI, Inna EP, Sanjai JP, Daniel AB. Microneedle-assisted delivery of verapamil hydrochloride and amlodipine besylate. Eur J Pharm Biopharm. 2014;86:284–91.

    Article  Google Scholar 

  17. Gomaa YA, Morrow DI, Garland MJ, Donnelly RF, El-Khordagui LK, Meidan VM. Effects of microneedle length, density, insertion time and multiple applications on human skin barrier function: assessments by transepidermal water loss. Toxicol in Vitro. 2010;24:1971–8.

    Article  CAS  PubMed  Google Scholar 

  18. Chueng K, Han T, Das DB. Effect of force of microneedle insertion on the permeability of insulin in skin. J Diabetes Sci Technol. 2014;8:444–52.

    Article  Google Scholar 

  19. Attia UM, Marsona S, Alcock JR. Micro-injection moulding of polymer microfluidic devices. Microfluidics and nano fluidics. 2009;7:1–28.

    Article  CAS  Google Scholar 

  20. Nair KJ, Whiteside BR, Grant C, Patel R, Tuinea-Bobe C, Norris K, Paradkar AR. Investigation of plasma treatment on micro-injection moulded microneedle for drug delivery. Pharmaceutics. 2015;7:471–85.

    Article  PubMed  PubMed Central  Google Scholar 

  21. Al-Qallaf B, Das DB, Mori D, Cui Z. Modelling transdermal delivery of high molecular weight drugs from microneedle systems. Phil Trans R Soc A. 2007;365:2951–67.

    Article  CAS  PubMed  Google Scholar 

  22. Leeladurga V, Teja UC, Ashraf SS, Sundeep K, Sai Sri Anusha V, Han T, Nalluri BN, Das DB. Application of microneedle arrays for enhancement of transdermal permeation of insulin: in vitro experiments, scaling analyses and numerical simulations. AAPS Pharma Sci Tech 2016;17(4):915–922.

  23. Vadim VY. US Patent No. 7658728 B2. Washington DC: U.S. Patent and Trademark Office; 2010.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Pharmaceutics, KVSR Siddhartha College of Pharmaceutical Sciences, Vijayawada, 520010 AP, India

    Buchi N. Nalluri, Chandrateja Uppuluri & Jyothirmayee Devineni

  2. Department of Chemical engineering, Loughborough University, Loughborough, LE11 3TU, UK

    Atul Nayak & Diganta B. Das

  3. Department of Engineering and Informatics, University of Bradford, Bradford, BD7 1DP, UK

    Karthik J. Nair & Benjamin R. Whiteside

Authors
  1. Buchi N. Nalluri
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Chandrateja Uppuluri
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Jyothirmayee Devineni
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Atul Nayak
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Karthik J. Nair
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. Benjamin R. Whiteside
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. Diganta B. Das
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Buchi N. Nalluri.

Ethics declarations

Conflict of interest

This study was funded jointly by the Department of Science and Technology (DST), Ministry of Science and Technology, Govt. of India, and the British Council, London, UK, under DST-UKIERI scheme (DST/INT/UK/P-60/2014) to Buchi N. Nalluri and Diganta B. Das. All 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

Nalluri, B.N., Uppuluri, C., Devineni, J. et al. Effect of microneedles on transdermal permeation enhancement of amlodipine. Drug Deliv. and Transl. Res. 7, 383–394 (2017). https://doi.org/10.1007/s13346-017-0361-z

Download citation

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s13346-017-0361-z

Keywords

Search

Navigation