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1、山竹素(mangostin)的透皮吸收康立峰，新加坡國立大學藥學系山竹素是山竹果皮提取物的主要活性成分之一。作為一個傳統(tǒng)的天然藥物，山竹素在東南亞地區(qū)廣泛應用于炎癥和感染性疾病的治療。本研究的目的是研制一個含山竹素的透皮制劑，用于治療關節(jié)疼痛，關節(jié)腫脹和關節(jié)炎。我們使用高效液相色譜法山對山竹素在各個配方溶液中的溶解度行了分析。在溶解度研究的基礎上，我們利用合成高分子薄膜確定了山竹素從各個配方溶液的釋放曲線。最后，通過水平擴散池實驗，我們確定了山竹素在各種配方溶液中的透皮速率。體外皮膚滲透實驗結(jié)果表明，可以通過添加化學皮膚滲透促進劑來增加山竹素的透皮擴散速率。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
