Preparation Of Lidocaine Ultradeformable Nano-Liposomes And The Studies On The Permeability Of It's As Transdermal Delivery

Liposome is a kind of occlusive bilayer vesicles which are formed of lipids such as phospholipids, the structure of which is similar to biological membranes,so it is also called artificial biological membranes. Liposome is an amphisome which can encapsulate both lipophilic drugs and hydrophilic drugs.As a vehicle, liposome can control the release of drugs, enhance the ability of targeting treatment, reduce side effects of drugs and increase the curative effect of drugs. In addition to this,liposome has also the tremendous deforming force,so it can be efficiently permeated into the systemic circulation through the unchanged stratum comeum while be got the strong stress. Ultradeformable liposomes added sodium cholate can preferably promote the penetration,so it is a new type of penetration enhancer. In this studies,we use lidocaine hydrochloride(LDH) as model drug which is lipophilic drug,but the significant permeability barrier of transdermal resorption is the stratum comeum,and ultradeformable liposomes can lower the effect of permeability barrier and enhance the drug delivery efficiency. Moreover, ultradeformable liposome as a new-type vehicle is extremely similar to the stratum comeum of skin on the composition and structure. Ultradeformable liposome can mix with stratum comeum so that increase the deposite of topical drug in skin, and then control the release of drug. In this experiment, LDH ultradeformable nano-liposomes have been prepared and it's skin penetration has been studied.Compared with the conventional liposomes, the effects of the ultradeformable liposomes is better by transdermal delivery.Chapter 1:Preparation and quality evaluation of LDH ultradeformable nano-liposomesOBJECT To prepare LDH ultradeformable nano-liposomes and evaluate its quality. METHODS Phosphatidylcholine and cholesterol were used as liposome materials, then sodium cholate as surface acting agent was added to, LDH ultradeformable nano-liposomes was prepared using a vacuum rotary evaporation method, the concentration of LDH was determined by high efficiency liquid chromatography. The morphology and the entrapment efficiency of LDH ultradeformable nano-liposomes were studied. RESULTS Mean diameter of the LDH ultradeformable nano-liposomes was (106±6.88)nm, The linear detection concentration range of LDH was 20-500μg/ml (r=0.99995) with average recovery at (100.4±0.44) % (n=3) and entrapment efficiency at (80.1±1.02)% (n=5). CONCLUSION This LDH ultradeformable nano-liposomes is feasible in preparation techniques, convenient and reliable in quality control method.Chapter 2:Studies on the permeability of LDH ultradeformable liposomes as transdermal deliveryOBJECT To study the permeability of LDH ultradeformable nano-liposomes as transdermal delivery through mouse skin and make additional comparison in penetrability between LDH ultradeformable nano-liposomes and conventional nano-liposomes. METHODS Use the High-performance liquid chromatographic methods to determine the contents of LDH in receptor solution, skin and blood of mice. To inspect accumulated concentrations of ultradeformable liposomes and conventional liposomes in modified Franz diffusion cell. RESULTS Velocity of permeability of ultradeformable liposomes is faster than that of conventional liposomes, and the percutaneous effect is better.CONCLUSION The surfactant can promote drugs to permeate into the skin. Ultradeformable nano-liposomes have deformability, so it can achieve the better saturate effect through its disfiguration in the action of aquatic resultant in skin.