Skip to main content
Article thumbnail
Location of Repository

Vesicular systems for delivering conventional small organic molecules and larger macromolecules to and through human skin

By Gamal M. El Maghraby and Adrian Christopher Williams

Abstract

The history of using vesicular systems for drug delivery to and through skin started nearly three decades ago with a study utilizing phospholipid liposomes to improve skin deposition and reduce systemic effects of triamcinolone acetonide. Subsequently, many researchers evaluated liposomes with respect to skin delivery, with the majority of them recording localized effects and relatively few studies showing transdermal delivery effects. Shortly after this, Transfersomes were developed with claims about their ability to deliver their payload into and through the skin with efficiencies similar to subcutaneous administration. Since these vesicles are ultradeformable, they were thought to penetrate intact skin deep enough to reach the systemic circulation. Their mechanisms of action remain controversial with diverse processes being reported. Parallel to this development, other classes of vesicles were produced with ethanol being included into the vesicles to provide flexibility (as in ethosomes) and vesicles were constructed from surfactants and cholesterol (as in niosomes). Thee ultradeformable vesicles showed variable efficiency in delivering low molecular weight and macromolecular drugs. This article will critically evaluate vesicular systems for dermal and transdermal delivery of drugs considering both their efficacy and potential mechanisms of action

Topics: 615
Publisher: Informa
Year: 2009
OAI identifier: oai:centaur.reading.ac.uk:4457

Suggested articles

Citations

  1. (2008). Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium doi
  2. (1998). Anti-inflammatory effects of Cu, Zn-superoxide dismutase in liposomes, Transfersomes or micelles, in the acute murine ear edema model.
  3. (1990). Antimicrob Agents Chemother doi
  4. (1996). Application of liposomes as potential cutaneous drug delivery systems. In vitro and in vivo investigation with radioactivity labelled vesicles.
  5. (2006). Can drug bearing liposomes penetrate intact skin? doi
  6. (2007). Cationic transfersomes based topical genetic vaccine against hepatitis B.
  7. (1992). Comedolytic activity of liposomal antiacne drug in an experimental model.
  8. (1997). Comparative topical anaesthesia of EMLA and liposome-encapsulated tetracaine.
  9. (1997). Corticosteroid dermal delivery with skin-lipid liposomes.
  10. (1993). Cutaneous bioavailability in hairless rats of tretinoin liposomes or gel.
  11. (1990). Dermal drug delivery by liposome encapsulation: Clinical and electron microscopic studies.
  12. (1983). Dermatological Formulations: Percutaneous Absorption,
  13. (2006). Development of novel fusogenic vesosomes for transcutaneous immunization. Vaccine
  14. (1992). Distribution of liposomeencapsulated ingredients in human skin ex vivo.
  15. (1987). Effect of egg yolk lecithin on transdermal delivery of bunazosin hydrochloride.
  16. (1988). Effects of phosphatidylcholine on the topical bioavailability of corticosteroids assessed by the human skin blanching assay.
  17. (1995). Effects of phospholipid based formulations on in vitro and in vivo percutaneous absorption of methyl nicotinate.
  18. (1996). Effects of phospholipids on the percutaneous penetration of indomethacin through the dorsal skin of the guinea pig, in vitro.
  19. (1996). Effects of phospholipids on the percutaneous penetration of indomethacin through the dorsal skin of the guinea pig, in vitro. 2. The effects of hydrophobic group in the phosphlipids and a comparison with general enhancers.
  20. (2002). Elastic liposomes for skin delivery of dipotassium glycyrrhizinate.
  21. (2006). Elastic liposomes mediated transcutaneous immunization against Hepatitis B. Vaccine
  22. (1997). Electron microscopic demonstration of the penetration of liposomes through skin. Folia Biol
  23. (2000). Enhanced delivery of drugs into and across the skin by ethosomal carriers. Drug Dev Res doi
  24. (2004). Enhanced transfollicular delivery of adriamycin with a liposome and iontophoresis. Exp Dermatol doi
  25. (2006). Enhancement of follicular delivery of finasteride by liposomes and niosomes. 1. In vitro permeation and in vivo deposition studies using hamster flank and ear models.
  26. (2000). Ethosomes – novel vesicular carriers for enhanced delivery: characterisation and skin penetration properties. doi
  27. (2007). Evaluation of uptake and generation of immune response by murine dendritic cells pulsed with hepatitis B surface antigen-loaded elastic liposomes. Vaccine,
  28. (1994). Follicular (pilosebaceous unit) deposition and pharmacological behavior of cimetidine as a function of formulation. Pharm Res
  29. (1991). How deep do intact liposomes penetrate into human skin?
  30. (2003). Hydration-driven transport of deformable lipid vesicles through fine pores and skin barrier.
  31. (1996). Imaging of transport pathways across human stratum corneum during high-voltage and low-voltage electrical exposures.
  32. (2007). Impact of antinucleants on transdermal delivery of testosterone from a spray. J Pharm Sci
  33. (1994). In vitro cutaneous and percutaneous delivery and in vivo effecacy of tetracaine from liposomal and conventional vehicles. Pharm Res
  34. (1984). Influence of liposomal drug entrapment on percutaneous absorption.
  35. (2002). Influence of microemulsions on cutaneous drug delivery, Advanced Drug Deliv Rev
  36. (1995). Interaction between liposomes and human stratum corneum in vitro: freeze fracture electron microscopical visualization and small angle X-ray scattering studies.
  37. (1995). Interaction of liposomes with human epidermis reconstructed in vitro.
  38. (1996). Interaction of liposomes with human skin in vitro - the influence of lipid composition and structure. Biochim Biophys Acta
  39. (1995). Interaction of phosphatidylcholine liposomes with the human stratum corneum. Biochim Biophys Acta
  40. (2004). Interactions of surfactants (edge activators) and skin penetration enhancers with liposomes.
  41. (1992). Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradients and hydration force. Biochim Biophys Acta
  42. (2002). Liposomal tacrolimus lotion as a novel topical agent for immune-mediated skin disorders: experimental studies in a murine model.
  43. (1992). Liposomally encapsulated active ingredients penetrate through the hair follicle.
  44. (1990). Liposome encapsulation improves efficacy of betamethasone dipropionate in atopic eczema but not in psoriasis vulgaris.
  45. (1999). Liposome-skin interactions and their effects on the skin permeation of drugs.
  46. (1994). Liposomes and niosomes as topical drug carriers: dermal and transdermal drug delivery. doi
  47. (1996). liposomes and other lipid suspensions on the skin: permeation enhancement, vesicle penetration, and transdermal drug delivery. Crit Rev Ther Drug Car Sys doi
  48. (2008). Liposomes and skin. From drug delivery to model membranes. doi
  49. (1985). Liposomes as a skin drug delivery system. doi
  50. (1992). Liposomes with clindamycin hydrochloride in therapy of acne vulgaris.
  51. (1982). Liposomes-a selective drug delivery system for topical route of administration: gel dosage form. doi
  52. (1980). Liposomes-a selective drug delivery system for topical route of administration. 1. lotion dosage form. Life Sci doi
  53. (1995). Material transport across the permeability barriers by means of lipid vesicles.
  54. (1994). Modulation of caffeine delivery by carrier design: liposomes versus permeation enhancers. doi
  55. (2005). Non-invasive vaccine delivery in transfersomes, niosomes and liposomes: a comparative study.
  56. (2005). Non-ionic surfactant based vesicles (niosomes) for non-invasive topical genetic immunization against hepatitis B.
  57. (1992). Noninvasive percutaneous induction of topical analgesia by a new type of drug carrier, and prolongation of local pain insensitivity by anesthetic liposomes. Aneth Analg
  58. (2001). Novel mechanisms and devices to enable successful transdermal drug delivery.
  59. (1995). Oestradiol permeation across human skin and silastic membranes: effects of propylene glycol and supersaturation. J Control Rel.
  60. (2000). Oestradiol skin delivery from ultradeformable liposomes: refinement of surfactant concentration.
  61. (2003). Particle size of liposomes influences dermal delivery of substance into skin.
  62. (2004). Penetration enhancers. Adv Drug Del Rev
  63. (1999). Percutaneous drug delivery to the hair follicle.
  64. (2003). Permeation of cyproterone acetate through pig skin from different vehicles with phospholipids.
  65. (1999). Phospholipids affect stratum corneum lipid bilayer fluidity and drug partitioning into the bilayers. J Control Rel
  66. (1982). Phospholipids as moisturizing agents.
  67. (2004). Quantitative assessment of the transport of elastic and rigid vesicle components and a model drug from these vesicle formulations into human skin in vivo. doi
  68. (1992). Rational for the production and dermal application of lipid vesicles.
  69. (1997). Sebaceous-gland deposition of isotretinoin after topical application: an in vitro study using human facial skin. Skin Pharmacol
  70. (2001). Skin delivery of 5-fluorouracil from ultradeformable and standard liposomes in vitro.
  71. (1999). Skin delivery of oestradiol from deformable and traditional liposomes: Mechanistic studies.
  72. (2000). Skin delivery of oestradiol from lipid vesicles: importance of liposome structure.
  73. (2001). Skin hydration and possible shunt route penetration in controlled skin delivery of estradiol from ultradeformable and standard liposomes in vitro. doi
  74. (2003). Skin penetration and mechanisms of action in the delivery of the D2-agonist rotigotine from surfactant-based elastic vesicle formulations. Pharm Res
  75. (1996). Synergistic effect of electric field and ultrasound on transdermal transport. Pharm Res
  76. (2008). Systemic and mucosal immune response induced by transcutaneous immunization using Hepatitis B surface antigen-loaded modified liposomes.
  77. (1997). Targeted and sustained delivery of hydrocortisone to normal and stratum corneum-removed skin without enhanced skin absorption using a liposome gel.
  78. (1996). Targeted delivery to pilosebaceous unit via liposomes. Advanced Drug Del Rev doi
  79. (1994). The influence of in vivo treatment of skin with liposomes on the topical absorption of a hydrophilic and a hydrophobic drug in vitro.
  80. (1994). The influence of particle size of liposomes on the disposition of drug into skin.
  81. (1996). The skin: a pathway for systemic treatment with patches and lipid-based agent carriers. Advanced Drug Del Rev.
  82. (1984). The use of liposomes in topical application of steroids.
  83. (1998). Topical anaesthesia of intact skin: Liposome-encapsulated tetracaine vs EMLA.
  84. (1988). Topical anesthesia of skin by liposome-encapsulated tetracaine. Aneth Analg
  85. (1992). Topical delivery enhancement with multilamellar liposomes into pliosebaceous units: I. In vitro evaluation using fluorescent techniques with hamster ear model. doi
  86. (1990). Topical delivery of cyclosporin: evaluation of various formulations using in vitro diffusion studies in hairless mouse skin. Skin Pharmacol doi
  87. (1992). Topical delivery of liposomally encapsulated gamma-interferon. Antiviral Res doi
  88. (1989). Topical delivery of liposomally encapsulated interferon evaluated in cutaneous herpes guinea pig model. Antimicrob Agents Chemother doi
  89. (2006). Topical delivery of low-molecular-weight heparinwith surface-charged flexible liposomes. Biomaterials
  90. (2003). Transdermal and Topical Drug Delivery; from theory to clinical practice.
  91. (2008). Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion: Effects of cosurfactants. doi
  92. (1995). Transdermal drug carriers: basic properties, optimization and transfer efficiency in the case of epicutaneously applied peptides.
  93. (1998). Transdermal immunisation with an integral membrane component, gap junction protein, by means of ultradeformable drug carriers, Transfersomes. Vaccine
  94. (1990). Transdermal iontophoresis of gonadotropin releasing hormone and two analogues.
  95. (1997). Transfersomes-mediated transepidermal delivery improves the regio-specificity and biological activity of corticosteroids in vivo.
  96. (1996). Triamcinolone permeation from different liposome formulations through rat skin in vitro.
  97. (1993). Ultra-high efficiency of drug and peptide transfer through the intact skin by means of novel drug-carriers, transfersomes.
  98. (2002). Ultradeformable lipid vesicles can penetrate skin and other semi-permeable membrane barriers unfragmented. Evidence from double label CLSM experiments and direct size measurement. Biochim Biophys Acta
  99. (1998). Ultraflexible vesicles, Transfersomes, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin. Biochim Biophys Acta
  100. (2003). Wouter Groenink HW, de Graaff AM, Bouwstra JA. The in vivo transport of elastic vesicles into human skin: effects of occlusion, volume and duration of application.

To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.