Researches on liposomes as vesicular drug delivery system.
S. number
Name and year of researchers
Drug
Experiment
Reference
01
Moghimipour et al., 2013
Triamcinolone acetonide
Liposomal gel of Triamcinolone acetonide were prepared to increase the deposition of drugs within the skin at the site of action and reduce side effects of drug using carbomer 940 as gelling agent. Four different gel formulations including hydroalcoholic, multilamellar large vesicles (MLV), small unilamellar vesicles (SUV), and blank MLV gel containing free drug were prepared. The in vitro drug release studies were determined using dialysis membrane method. The results of drug release showed that SUV liposomal gel has the most regular and the least interaction between the drug and polymer.
Sustained release liposomes of Metformin hydrochloride were prepared using film hydration technique using varying concentrations of phosphatidylcholine and cholesterol. The results of in vitro drug release studies showed that release from liposomal formulation followed first order kinetics and sustained for >12 hrs. The release mechanism was non-Fickian diffusion from all the formulations.
Sustained release liposomes of Salbutamol sulfate were prepared using soya lecithin and cholesterol for the treatment of asthma. The results of in vitro dissolution studies exhibited drug release 96.24% in 12 h and the total release pattern was very close to the theoretical release profile of sustained release system. No significant difference in drug release profile was observed during the stability study period of 2 months.
Liposomes of Acyclovir were prepared for enhanced oral bioavailability using various ratios of phosphatidylcholine with cholesterol and Cephalin (phosphatidylethanolamine) with cholesterol by reverse phase evaporation method. The % entrapped drug in soya lecithin liposomes was 60.51% and sustained the release and at the end of 12 hr the % drug release was 73.89%. The liposomes stored at 4°C were found to be stable for duration of two months compared to other storage conditions.
Liposomes of Pentoxifylline were prepared for enhanced oral bioavailability. The formulation showed release up to 8 h and above 90% of drug was released. The drug release kinetics was governed by Peppas model. It was concluded that as the percentage of cholesterol increased there was subsequent increase in the stability and rigidity of liposomes but at the same time percentage drug entrapment was reduced due to reduction in phosphatidylcholine and as the concentration of cholesterol increases, the particle size increases which was maybe due to formation of rigid bilayer structure.
Liposomes of Ketoconazole were prepared for topical application. The drug entrapment efficiency was found to be 54.41 ± 0.19%. The percentage cumulative drug release was determined by diffusion studies and found to be 34.96 ± 0.86% after 12 hours. Stability studies present percent drug retention at refrigerated temperature (2–8°C).
Dianthrol was entrapped in vesicles to help in the localized delivery of the drug and to improve availability of the drug at the site to reduce the dose and, in turn, the dose-dependent side effects like irritation and staining. The mean liposome and niosomes sizes were 4 ± 1.25 and 5 ± 1.5 m, respectively. The drug-leakage study carried out at different temperatures of 4–8, 25 ± 2, and 37°C for a period of two months affirms that the drug leakage increased at a higher temperature. The in vitro permeation study using mouse abdominal skin showed significantly enhanced permeation with vesicles as indicated by flux of Dianthrol from liposomes (23.13 g/cm2/h) and niosomes (7.78 g/cm2/h) as compared with the cream base (4.10 g/cm2/h).
The liposomes of the drug were prepared to reduce the toxic side effects such as ulceration of the kidney and central nervous system (CNS) toxicity. The drug release profile from the liposomes was biphasic, and the highest percentage drug release was observed with large unilamellar vesicles (LUVs) (100 nm). The anti-inflammatory activity was increased from the first to fifth hour PC : CH : PG (1 : 0.5 : 0.2) and PC : CH : SA (1 : 0.5 : 0.1) liposomes showed the highest percentage inhibition of edema. The ulcer index of the free drug was about three times more than the encapsulated drug when administered at the same dose intraperitoneally to arthritic rats consecutively for 21 days.
Liposome gels bearing an antineoplastic agent, 5-Fluorouracil, intended for topical application have been prepared. Liposomes were prepared by the film hydration method by varying the lipid phase composition (PL 90H/cholesterol mass ratio) and hydration conditions of dry lipid film (drug/aqueous phase mass ratio). Topical liposome gels were prepared by incorporation of lyophilized liposomes into a structured vehicle (1%, m/m, chitosan gel base). The rate of drug release from liposome gels was found to be dependent on the bilayer composition and the dry lipid film hydration conditions. The drug release obeyed the Higuchi diffusion model, while liposomes acted as reservoir systems for continuous delivery of the encapsulated drug.
Melatonin loaded liposomes were prepared and were found to be spherical, unilamellar structures having low polydispersity (0.032 ± 0.011) and nanometric size range (122 ± 3.5 nm). % entrapment efficiency of drug in ethosomal carrier was found to be 70.71 ± 1.4. Stability profile of prepared system assessed for 120 days revealed very low aggregation and growth in vesicular size (7.6 ± 1.2%). MT loaded ethosomal carriers also provided an enhanced transdermal flux of 59.2 ± 1.22 g/cm2/h and decreased lag time of 0.9 h across human cadaver skin
