The objective of this study was to synthesize and characterize a series of novel diblock copolymer containing sugar moiety at a terminal group as a transdermal penetration enhancer. Sugar-based micelles are advantageous because they are highly biodegradable and non-toxic. Those amphiphilic diblock copolymers may be regarded as a building block for the micellar drug carriers and cosmetic delivery systems. Normally transdermal permeation enhancers are of relatively low molecular weight, probability that they permeate through the skin and cause unfavorable side effects. Polymeric transdermal enhancers may exhibit a high enhancing activity and non-toxic due to the bulkiness of enhancer and the physiological inertness. The enhancing activity of poly(lactic acid) end-capped lactose (PLL), poly(lactic acid)-b-hyaluronan (PLH) on the permeation through the nude mice dorsum skin were evaluated by in vitroexperiments using a franz cell and lidocaine chloride as a model drug. As a result, PLL exhibited a higher enhancing effect on the permeation the drug through the skin, which may suggested that a suitable balance of polarity and hydrophobicity of the penetration enhancers would be necessary to appear the high enhancing effect.

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