Improvement of dermal delivery of tetracycline using vesicular nanostructures

Azam Hasanpouri , Farzaneh Lotfipour, Saeed Ghanbarzadeh, Hamed Hamishehkar


The objective of this investigation was to study the potential use of nanoliposomes and nanotransfersomes in dermal delivery of tetracycline hydrochloride (TC) for acne treatment. Vesicular nanostructures were prepared by thin film hydration method and evaluated for their size, zeta potential, morphology, and entrapment efficiency. Minimal inhibitory concentration values of TC-loaded vesicles were evaluated and compared with TC aqueous solution against Staphylococcus epidermis. In vitro drug release and ex vivo drug permeation through the excised rat skin were performed to assess drug delivery efficiency. Particle size, zeta potential, and entrapment efficiency of prepared nanoliposomes and nanotransfersomes were found to be 75 and 78 nm, 17 and 7 mV, and 45 and 55%, respectively. Antimicrobial analysis indicated that there was no difference between vesicular formulations and aqueous solution of TC. In vitro drug release study indicated that nanoliposomes could release TC 2.6 folds more than nanotransfersomes, and skin permeation study showed that the permeability of TC-loaded nanotransfersomes was 1.6 times higher than nanoliposomes which was also confirmed by fluorescence microscope imaging. These findings concluded that nanoliposomal and especially nanotransfersomal formulations could be proposed as the potential approach for better therapeutic performance of TC against acne.


Acne; Dermal drug delivery; Liposome; Nanoparticle; Tetracycline; Transferosome.

Full Text:



Goyal R, Macri LK, Kaplan HM, Kohn J. Nanoparticles and nanofibers for topical drug delivery. J Control Release. 2016;240:77-92.

Pham QD, Björklund S, Engblom J, Topgaard D, Sparr E. Chemical penetration enhancers in stratum corneum - Relation between molecular effects and barrier function. J Control Release. 2016;232: 175-187.

Mahto A. Acne vulgaris. Medicine. 2017;45(6): 386-389.

Nagler AR, Milam EC, Orlow SJ. The use of oral antibiotics before isotretinoin therapy in patients with acne. J Am Acad Dermatol. 2016;74(2): 273-279.

Rahimpour Y, Javadzadeh Y, Hamishehkar H. Solid lipid microparticles for enhanced dermal delivery of tetracycline HCl. Colloids Surf B Biointerfaces. 2016;145:14-20.

Akhtar N, Khan RA. Liposomal systems as viable drug delivery technology for skin cancer sites with an outlook on lipid-based delivery vehicles and diagnostic imaging inputs for skin conditions'. Prog Lipid Res. 2016;64:192-230.

Hamishehkar H, Shokri J, Fallahi S, Jahangiri A, Ghanbarzadeh S, Kouhsoltani M. Histopathological evaluation of caffeine-loaded solid lipid nanoparticles in efficient treatment of cellulite. Drug Dev Ind Pharm. 2015;41(10):1640-1646.

Rahimpour Y, Hamishehkar H. Liposomes in cosmeceutics. Expert Opin Drug Deliv. 2012;9(4):443-455.

Hamishehkar H, Rahimpour Y, Kouhsoltani M. Niosomes as a propitious carrier for topical drug delivery. Expert Opin Drug Deliv. 2013;10(2): 261-272.

Elron-Gross I, Glucksam Y, Margalit R. Liposomal dexamethasone-diclofenac combinations for local osteoarthritis treatment. Int J Pharm. 2009; 376(1-2):84-91.

Manconi M, Mura S, Sinico C, Fadda AM, Vila AO, Molina F. Development and characterization of liposomes containing glycols as carriers for diclofenac. Colloids Surf Physicochem Eng Aspects. 2009;342(1-3):53-58.

Al Shuwaili AH, Rasool BK, Abdulrasool AA. Optimization of elastic transfersomes formulations for transdermal delivery of pentoxifylline. Eur J Pharm Biopharm. 2016;102:101-114.

Hassanpour Aghdam M, Ghanbarzadeh S, Javadzadeh Y, Hamishehkar H. Aggregated nanotransfersomal dry powder inhalation of itraconazole for pulmonary drug delivery. Adv Pharm Bull. 2016;6(1):57-64.

Hamishehkar H, Same S, Adibkia K, Zarza K, Shokri J, Taghaee M, et al. A comparative histological study on the skin occlusion performance of a cream made of solid lipid nanoparticles and Vaseline. Res Pharm Sci. 2015;10(5):378-387.

Ghanbarzadeh S, Hariri R, Kouhsoltani M, Shokri J, Javadzadeh Y, Hamishehkar H. Enhanced stability and dermal delivery of hydroquinone using solid lipid nanoparticles. Colloids Surf B Biointerfaces. 2015;136:1004-1010.

Mokarizadeh M, Kafil HS, Ghanbarzadeh S, Alizadeh A, Hamishehkar H. Improvement of citral antimicrobial activity by incorporation into nanostructured lipid carriers: a potential application in food stuffs as a natural preservative. Res Pharm Sci. 2017;12(5):409-415.

Kang L, Yap CW, Lim PF, Chen YZ, Ho PC, Chan YW, et al. Formulation development of transdermal dosage forms: quantitative structure-activity relationship model for predicting activities of terpenes that enhance drug penetration through human skin. J Control Release. 2007;120(3): 211-219.

Cronin M, Dearden JC, Moss GP, Murray-Dickson G. Investigation of the mechanism of flux across human skin in vitro by quantitative structure-permeability relationships. Eur J Pharm Sci. 1999;7(4):325-330.

Zhang GH, Zhao CY. Synthesis and characterization of a narrow size distribution nano phase change material emulsion for thermal energy storage. Sol Energy. 2017;147:406-413.

Zandi G, Lotfipour F, Ghanbarzadeh S, Medghalchi M, Hamishehkar H. A comparative study on the potentials of nanoliposomes and nanoethosomes for Fluconazole delivery. J Drug Deliv Sci Technol. 2018;44:264-269.

Heydari S, Ghanbarzadeh S, Anoush B, Ranjkesh M, Javadzadeh Y, Kouhsoltani M, et al. Nanoethosomal formulation of gammaoryzanol for skin-aging protection and wrinkle improvement: a histopathological study. Drug Dev Ind Pharm. 2017;43(7):1154-1162.

Chaudhary H, Kohli K, Kumar V. Nano-transfersomes as a novel carrier for transdermal delivery. Int J Pharm. 2013;454(1):367-380.

Cevc G. Rational design of new product candidates: the next generation of highly deformable bilayer vesicles for noninvasive, targeted therapy. J Control Release. 2012;160(2):135-146.

Mugglestone CJ, Mariz S, Lane ME. The development and registration of topical pharmaceuticals. Int J Pharm. 2012;435(1):22-26.

Zhai Y, Zhai G. Advances in lipid-based colloid systems as drug carrier for topic delivery. J Control Release. 2014;193:90-99.

Gupta R, Rai B. Effect of size and surface charge of gold nanoparticles on their skin permeability: A molecular dynamics study. Sci Rep. 2017;7: 45292-45304.

Pinto-Alphandary H, Andremont A, Couvreur P. Targeted delivery of antibiotics using liposomes and nanoparticles: research and applications. Int J Antimicrob Agents. 2000;13(3):155-168.

Chorachoo J, Amnuaikit T, Voravuthikunchai SP. Liposomal encapsulated rhodomyrtone: a novel antiacne drug. Evid Based Complement Alternat Med. 2013;2013. Article ID: 157635. DOI: 10.1155/2013/157635.

Ballottin D, Fulaz S, Cabrini F, Tsukamoto J, Durán N, Alves OL, et al. Antimicrobial textiles: Biogenic silver nanoparticles against Candida and Xanthomonas. Mater Sci Eng C. 2017;75:582-589.

Chang TY, Chen CC, Cheng KM, Chin CY, Chen YH, Chen XA, et al. Trimethyl chitosan-capped silver nanoparticles with positive surface charge: Their catalytic activity and antibacterial spectrum including multidrug-resistant strains of Acinetobacter baumannii. Colloids Surf B Biointerfaces. 2017;155:61-70.

Mohamed MM, Fouad SA, Elshoky HA, Mohammed GM, Salaheldin TA. Antibacterial effect of gold nanoparticles against Corynebacterium pseudotuberculosis. Int J Vet Sci Med. 2017;5(1):23-29.


  • There are currently no refbacks.

Creative Commons Attribution-NonCommercial 3.0

This work is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License which allows users to read, copy, distribute and make derivative works for non-commercial purposes from the material, as long as the author of the original work is cited properly.