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1、山竹素(mangostin)的透皮吸收康立峰，新加坡国立大学药学系山竹素是山竹果皮提取物的主要活性成分之一。作为一个传统的天然药物，山竹素在东南亚地区广泛应用于炎症和感染性疾病的治疗。本研究的目的是研制一个含山竹素的透皮制剂，用于治疗关节疼痛，关节肿胀和关节炎。我们使用高效液相色谱法山对山竹素在各个配方溶液中的溶解度行了分析。在溶解度研究的基础上，我们利用合成高分子薄膜确定了山竹素从各个配方溶液的释放曲线。最后，通过水平扩散池实验，我们确定了山竹素在各种配方溶液中的透皮速率。体外皮肤渗透实验结果表明，可以通过添加化学皮肤渗透促进剂来增加山竹素的透皮扩散速率。2Intr
2、oductionNaturalantioxidantsfromplantextractshavegainedsignificantattentionduetoconsumerconcernaboutthesafetyofthesyntheticcompounds.Antimutagenic,antioxidantandanticarcinogenicactivitiesofextractsfromfruits,vegetablesandcerealshavebeenreported[1].Recently,extractsoffruits,vegetables,her
3、bs,cereals,sproutsandseeds[2]havebeenshowntohaveantioxidantactivityindifferentmodelsystems.MangostinfromtheextractsofthefruitrindsofG.mangosteenwasshowntopossessantioxidantandantimutagenicproperties[3].Theα-mangostin(Figure1),oneofamajoractivexanthonoidfromthefruitrindextractofmangostee
4、n,wasreportedtorelievejointpain[4].Inthisstudy,weaimtodelivermangostinaslocalanalgesicsthroughskin.Figure1Thechemicalstructuresofα-mangostinandβ-mangostin.Currently,nonsteroidalanti-inflammatorydrugs(NSAIDs)aretheactiveingredientsinmosttopicalanalgesics.Whilepossessinganti-inflammatorye
5、ffect,NSAIDsalsohavemanyundesirableside-effects,suchasgastrointestinalirritationandbleeding[5].Besides,salicylatederivatives,forexamplemethylsalicylate,istoxicifappliedaboveacertainamount[6].Inviewoftheundesirablesideeffectsoftraditionalsalicylates,mangostinmaybepreferredasitissaferandw
6、ithlesssideeffects[7].Thedevelopmentoftopicaldrugdeliverysystemsisadvisableandbeneficialduetoseveraladvantages,suchasreducedsystemictoxicityandtargeteddelivery[8].However,onlylimitedamountofdrugcanpermeatethroughskin,duetotherelativeimpermeabilityofskin[9].Therefore,extensivepre-formula
7、tionstudiesaregenerallynecessaryinordertooptimizebothdrugreleasefromtopicalvehicleandskinpermeation[10].Inthisstudy,topicalα-mangostininseveralformulationswasinvestigated.ThesolubilityofmangostinindifferentmediumswasdeterminedbyusingaHPLCmethod.Thepermeationprofilesofthedrugthr
