Vesicular system: Versatile carrier for transdermal delivery of bioactives

Figures & data

Figure 1. Different routes of drug transport through skin.

Table I. List of vesicular carriers used for transdermal drug delivery.

S. No.	Vesicular systems	Advantage	Disadvantage	References
1.	Emulsomes	High systemic targeting property, low dose of drug is required hence preventing dose-related adverse effect	High production cost	Gill et al. (2012)
2.	Enzymosomes	Increased stability, reduction in toxicity of the encapsulated agent, and improved pharmacokinetic effect (increase circulation time)	High production cost, leakage, and fusion of encapsulated drug molecules	Tadwee et al. (2012)
3.	Virosomes	Biodegradable, biocompatible, nontoxic, promote fusion activity in endosomal pathway, and protect drugs against degradation	Limited bioactives can be delivered	Patel et al. (2010)
4.	Ethosomes	Delivery of large molecules (peptides, protein molecules) is possible	Skin irritation due to excipients and enhancers of drug delivery systems	Godin and Touitou (2003)
5.	Liposomes	Reduces exposure of sensitive tissues to toxic drugs, biodegradable, and nontoxic, and thus avoiding systemic/local side effects	Leakage and fusion of encapsulated drug molecules, chances of oxidation, and hydrolysis of phospholipids	Jones and Moss (2010)
6.	Pharmacosomes	Suitable for incorporating both hydrophilic and lipophilic drugs, no need of following the tedious, time-consuming step for removing the free, unentrapped drug from the formulation. Oral, topical, extra- or intravascular delivery is possible	Required covalent bonding to protect the leakage of drugs on storage, undergo fusion and aggregation, as well as chemical hydrolysis	Semalty et al. (2009)
7.	Transferosomes	It can accommodate drug molecules with wide range of solubility	Expensive and chemically unstable because of their predisposition to oxidative degradation	Kulkarni et al. (2011)
8.	Niosomes	It is biodegradable, biocompatible and nonimmunogenic to the body, controlled, and sustained release of drugs due to depot formation	Physical instability during storage due to vesicles aggregations and low entrapment	Khan et al. (2011)
9.	Sphingosomes	Flexibility to couple with site-specific ligands to achieve active targeting, improve pharmacokinetic effect, and increase efficacy and stability	High production cost	Saraf et al. (2011)

Figure 2. Percutaneous penetration of lipid vesicular carrier.

Table II. List of vesicular carriers used for transdermal delivery of bioactives.

S. No.	Delivery system	Bioactive used	Method used	Remark	References
1.	Liposomes	Ketoprofen	Sonication	Surfactant-based liposomes enhanced ketoprofen transport across human skin	Uchino et al. (2013)
		Clotrimazole	Rotary evaporation method	Higher skin permeation andenhanced antifungal activity of optimized elastic liposomes	Kumar et al. (2011)
		Paroxetine	Reverse-phase evaporation method	Improved bioavailability of the Paroxetine after liposomal transdermal patch application and sustaining of the therapeutic effects compared to oral administration	El-Nabarawi et al. (2013)
		Amphotericin B (AmBisome)	Modified ethanol-injection method	AmB showed no sign of degradation in reconstituted liposomes stored at 2–8°C for more than 3 months	Singodia et al. (2012)
		Recombinant human epidermal growth factor (rhEGF)	High-pressure homogenization method	Enhanced the permeation and localization of rhEGF in rat skin by facilitating entry through pores of skin	Jeon et al. (2012)
2.	Transferosome	Insulin	Reverse-phase evaporation method	Prolonged hypoglycemic effect in diabetic rats over 24 h after transdermal administration	Malakar et al. (2012)
		Sertraline	Rotary evaporation method	Transferosomal drug exhibited better antidepressant activity as compared to the plain drug	Gupta et al. (2012)
		Ketoconazole	Lipid film hydration technique	Transferosomal formulation improved the release and permeation of Ketokonazole	Rajan and Vasudevan (2012)
3.	Niosomes	Sumatriptan succinate	Thin-film hydration method	Successfully optimized sumatriptan succinate niosomes as drug carriers for skin delivery	Gonzalez-Rodriguez et al. (2012)
		Papain	Thin-film hydration method	Enhanced transdermal absorption of papain rat skin and the improvement of scar reduction in rabbit ear model	Manosroi et al. (2013)
		Tyrosinase gene	Freeze-dried empty liposomes method	Enhanced expression of human tyrosinase gene by loading in elastic cationic niosomes, but also the potential application of this gene delivery system for the further development of vitiligo gene therapy	Khositsuntiwong et al. (2012)
		Fluconazole	Film hydration method	Sustained release with enhanced cutaneous retention of the drug	Gupta et al. (2011)
		Rofecoxib	Lipid film hydration technique	As compared to plain drug gel, niosomal gel assured the prolong drug release behavior with sustained action across pig skin	Das and Palei (2011)
4.	Ethosomes	Econazole nitrate	Cold method	controlled drug release, better antifungal activity, and good storage stability	Verma and Pathak (2012)

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