Review Article

Lipid Based Vesicular Drug Delivery Systems

Table 2

Researches on niosomes as vesicular drug delivery system.

S. numberName and year of researchersDrugExperimentReference

01Parthibarajan
et al., 2013
VoriconazoleVoriconazole niosomes were prepared by hand shaking and ether injection method using span 80 and cholesterol. The niosomes size range was 0.5–5  and 0.5–2.5  by hand shaking method and ether injection method, respectively. The percent entrapment efficiency of niosomal formulation containing Voriconazole was determined by dialysis method. The drug entrapment efficiency was found to be more than 84.53% in case of niosomes prepared by hand shaking process. The in vitro release profile of drug indicated 70.06% drug release extended period of 24 hours for the formulation prepared by hand shaking method.[27]

02Allam et al., 2011AcyclovirOphthalmic niosomes of Acyclovir were prepared using two different methods, that is, film hydration method (FHM) and reverse phase evaporation method (REV). Particle size distribution studies showed that particle size was the smallest in absence of cholesterol and as the amount of cholesterol was increased, subsequent increase in particle size was observed. Corneal permeation studies showed that the cumulative amount permeated from most niosomal formulations was lower than that from solution containing drug, except the formulations having cholesterol: surfactant molar ratio 1 : 1. No corneal damage was observed during corneal hydration studies. Prepared niosomes were more stable at 4°C than at 25°C.[28]

03 Sathyavathi et al., 2012Brimonidine tartrateNiosomal in-situ gel of Brimonidine tartrate was developed using different ratios of span series and cholesterol for improved ocular bioavailability for the treatment of glaucoma. Small unilamellar vesicles were prepared in the size range of 50–100 nm. The niosomal formulation was transformed into gel when it was instilled into the eye. All the formulations exhibited pseudoplastic rheological behavior and slow drug release pattern. Antiglaucoma activity of the prepared gel formulations showed more significant and sustained effect in reducing intraocular pressure than marketed and niosomal drops.[29]

04Rani et al., 2010 Rifampicin and gatifloxacinNiosomes of rifampicin and gatifloxacin were prepared by lipid hydration technique using rotary flash evaporator. The prepared niosomes showed a vesicle size in the range of 100–300 nm, the entrapment efficiency was 73% and 70%, respectively. The in vitro release study showed 98.98% and 97.74% of release of rifampicin and gatifloxacin niosomes, respectively. The bactericidal activities of prepared formulation were studied by BACTEC radiometric method using the resistant strains (RF 8554) and sensitive strains (H37Rv) of Mycobacterium tuberculosis which showed greater inhibition and reduced growth index.[30]

05Ning et al., 2005ClotrimazoleNiosomes were evaluated as delivery vehicles to develop alternative formulation for the vaginal administration of clotrimazole, to provide sustained and controlled release of appropriate drug for local vaginal therapy. Niosomes were prepared by lipid hydration method and were incorporated into 2% carbopol gel, and the systems were evaluated for drug stability in phosphate-buffered saline (pH 7.4) and simulated vaginal fluid at 37 ± 1°C. Further, the vesicle gel system was evaluated by antifungal activity and tolerability on tissue level in rat.[31]

06Mura et al., 2007MinoxidilMinoxidil loaded niosomes were formulated to improve skin drug delivery. Multilamellar niosomes were prepared using soya phosphatidylcholine. Minoxidil skin penetration and permeation experiments were performed in vitro using vertical diffusion franz cells and human skin treated with either drug vesicular systems or propylene glycol-water-ethanol solution (control). Penetration of Minoxidil in epidermal and dermal layers was greater with liposomes than with niosomal formulations and the control solution. The greatest skin accumulation was always obtained with nondialyzed vesicular formulations. No permeation of Minoxidil through the whole skin thickness was detected in the present study. It was concluded that alcohol-free liposomal formulations would constitute a promising approach for the topical delivery of Minoxidil in hair loss treatment.[32]

07 Guinedi et al., 2005AcetazolamideNiosomes were prepared by reverse-phase evaporation and thin film hydration method using Span 40 or Span 60 and cholesterol in the molar ratios of 7 : 4, 7 : 6 and 7 : 7. Stability studies were carried out to investigate the leaching of drug from niosomes during storage. It was observed that the type of surfactant, cholesterol content, and the method of preparation altered the entrapment efficiency and drug release rate from niosomes. Higher entrapment efficiency was obtained with multilamellar niosomes prepared from Span 60 and cholesterol in a 7 : 6 molar ratio. Niosomal formulations have shown a fairly high retention of Acetazolamide inside the vesicles (approximately 75%) at a refrigerated temperature up to a period of 3 months. Multilamellar Acetazolamide niosomes formulated with Span 60 and cholesterol in a 7 : 4 molar ratio were found to be the most effective and showed prolonged decrease in intraocular pressure.[33]

08Ruckmani et al., 2000Cytarabine hydrochlorideNiosome vesicles of Cytarabine hydrochloride were prepared by a lipid hydration method that excluded dicetylphosphate. The sizes of the vesicles obtained ranged from 600 to 1000 nm, with the objective of producing more blood levels in vivo. The study of the release of drug from niosomes exhibited a prolonged release profile as studied over a period of 16 hr. The drug entrapment efficiency was about 80% with Tween 80, Span 60, and Tween 20; for Span 80, it was 67.5%. The physical stability profile of vesicular suspension was good as studied over a period of 4 weeks.[34]