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PART 2 Kev Npaj Thiab Kev Ntsuas Ntawm Microemulsion-based Transdermal Delivery Of Cistanche Tubulosa Phenylethanoid Glycosides

Mar 06, 2022

Hu rau: Audrey Hu Whatsapp / hp: 0086 13880143964 Email:audrey.hu@wecistanche.com

Nyem qhov no mus rau PART 1

Rau cov tshuaj molecules, thiab ua rau muaj kev tso tawm sai dua nrog lub diffusion-tswj tso tawm mechanism (29). Qhov permeation-txhim kho cov nyhuv ntawm IPM tuaj yeem ua rau kom muaj qhov sib txawv ntawm PG(Phenylethanoild glycoside los ntawm cistanche)-loaded ME nyob rau hauv cov ntaub so ntswg ntawm daim tawv nqaij, uas yuav ua rau kom muaj permeation coefficient (30). Tsis tas li ntawd, cov ntsiab lus dej ntawm MEs tuaj yeem txhim kho permeation raws li hydration ntawm stratum corneum pab txhawb kev txhim kho thiab nthuav dav ntawm cov channel hauv keratin txheej thiab qhov cuam tshuam ntawm lipid bilayer (24). Hauv kev tshawb fawb tam sim no, cov ntsiab lus dej hauv ME5 (65 feem pua) tau siab dua li lwm cov MEs (Table I), txhais tau tias ME5 tuaj yeem ua rau muaj qhov permeation ntau dua. Tsis tas li ntawd, qhov loj me me tuaj yeem cuam tshuam rau permeation profiles, uas yogME nrog cov tee me me tuaj yeem ua rau daim tawv nqaij permeation. Muab ua ke, ME5 formulated nrog qhov tsim nyog tus nqi ntawm surfactant sib tov (28 feem pua) thiab dej (65 feem pua), nrog me me droplet loj (30.56 nm) thiab tsawg viscosity (30.43 mPa.s), qhia tau zoo permeability piv nrog rau lwm yam ME formulations .

CISTANCHE

Tus nqi ntawm PG(Phenylethanoild glycoside los ntawm cistanche)uas nkag mus rau ntawm daim tawv nqaij nce nrog kev thauj tshuaj (Daim duab 6). Tsis tas li ntawd, kev siv tshuaj ntau ntxiv ua rau muaj kev txhawb nqa ntawm kev xa tshuaj transdermal (24,31). Rau ME5, 6. . 6) piv nrog 0.5 feem pua ​​​​cov tshuaj thauj khoom (35.504 µg/cm-2 /h-1 ; Fig. 6). Txawm li cas los xij, vim lub cev tsis ruaj khov ntawm 3.0 feem pua ​​​​cov tshuaj thauj khoom, uas ua rau lub crystallization ntawm PG thaum lub sij hawm cia, qhov kawg loading ntawm PG.(Phenylethanoild glycoside los ntawm cistanche)hauv ME5 yog 2.0 feem pua ​​. Kev sib piv ntawm qhov optimized ME thiab PG aqueous tov yog tso tawm nyob rau hauv Table IV. A 1. Qhov sib npaug ntawm PG hauv pawg ME uas tau txais txiaj ntsig zoo (4149.650 ± 37.3 µg·cm-2 ) tau nce ntau dua pivnrog PG(Phenylethanoild glycoside los ntawm cistanche)saline pab pawg (2288.63±20.9 µg•cm-2, P=0.0039; Table IV) Cov permeability coefficient qhia tias qhov optimized ME (8.87± 0.49 cm/h; Table IV) kuj tau nce ntxiv piv nrog PG saline tov [5.41 ± 0.12 (cm / h) x10-3; P=0.041; Table IV], tawm tswv yim tias optimized ME yog ib qho kev ua haujlwm zoo ntawm PG(Phenylethanoild glycoside los ntawm cistanche)tshaj saline. Raws li cov ntaub ntawv dhau los (16,32), siab concentration (2 feem pua) ntawm PG hauv MEs ua rau muaj qhov siab concentration gradient, uas ua rau cov permeation ntawm PG rau ntawm daim tawv nqaij. MEs tuaj yeem ua raws li cov dej ntim tshuaj, nrog rau cov tshuaj raug tso tawm los ntawm theem sab hauv mus rau sab nrauv thiab tom qab ntawd mus rau ntawm daim tawv nqaij. Tsis tas li ntawd, MEs tuaj yeem cuam tshuam rau cov qauv stratum corneum thiab txo qhov cuam tshuam ntawm diffusional los ntawm kev ua tus permeation enhancer (26,33). Kev tshawb nrhiav tawv nqaij. Kev ua kom zoo rau ME hauv txoj kev tshawb fawb tam sim no tau pom tias muaj peev xwm tso tshuaj ntau dua li PG aqueous tov (174.07 ± 1.51 µg·cm-2 vs. 93.25± 1.49 µg·cm-2; P=0 .029, Tab IV). Qhov no tuaj yeem cuam tshuam nrog kev tso tawm sai ntawm PG los ntawm kev ua kom zoo rau ME, uas ua rau kom cov tshuaj nkag mus rau hauv daim tawv nqaij, lossis kom muaj kev solubility ntau dua ntawm qhov optimized ME piv nrog PG saline tov. Vim qhov no tshwm sim, qhov nce ntawm PG yog khaws cia hauv daim tawv nqaij.

Phenylethanoild glycoside from cistanche


Qhov kev ua kom zoo tshaj plaws ntawm ME5 pom tau tias cov tawv nqaij ruaj khov dua li PG(Phenylethanoild glycoside los ntawm cistanche)saline daws (30). Qhov optimized ME kuj zoo dua rau PG saline tov cov ntsiab lus ntawm daim tawv nqaij permeation profiles thiab daim tawv nqaij tuav (Table IV). Ua ke, qhov ua kom zoo tshaj ME xa PG zoo dua li PG saline tov. Kev kawm ruaj khov. Cov kev tshawb fawb txog kev ruaj ntseg tau ua los xyuas seb muaj kev hloov pauv hauv pH, qhov loj me me, thiab cov ntsiab lus ntawm cov tshuaj. Optimized ME yog lub cev ruaj khov (16,29) khaws cov homogeneity thiab tsis pom kev sib cais tom qab 3 lub hlis. Tsis muaj kev hloov pauv loj tau pom nyob rau hauv qhov loj me me thiab qhov degradation ntawm PG hauv 3 lub hlis. Cov kev ntsuam xyuas centrifuge pom tau tias optimized ME yog lub cev ruaj khov. Tsis muaj kev hloov pauv tseem ceeb tau sau tseg hauv ME khaws cia, tab sis muaj qhov txo qis me ntsis hauv viscosity. Qhov kev txo qis no tuaj yeem yog vim qhov poob dej thaum khaws cia. Peb lub hlis tom qab, tsis muaj qhov sib txawv ntawm pH, qhov loj me me, cov ntsiab lus ntawm cov tshuaj thiab viscosity ntawm ME khaws cia ntawm 2-8˚C thiab ntawm chav tsev kub (Table V). Kev kuaj tawv nqaij rhiab heev. Qhov kev siv zog ntawm daim tawv nqaij khaus ua raws li cov txheej txheem, thiab cov qhab nia ntawm<0.5 meant="" no="" irritation,="" 0.5-3="" slight="" irritation,="" 3-6="" moderate="" irritation,="" and="">6 mob hnyav heev. Cov tsos mob me me tau pom nyob rau hauv cov tsiaj kho nrog optimized ME.

Qhov nruab nrab cov qhab nia ntawm cov tawv nqaij khaus rau cov kua qaub nrog 2 feem pua ​​(w/w) PG(Phenylethanoild glycoside los ntawm cistanche)yog {{0}}.1±0.05, 0.1±{{10}}.13, thiab {{ 17}}.1±{19}} 07 ntawm 24, 48 thiab 72 h, raws Rau qhov optimized ME, cov qhab nia yog 0.28±{25}}.02, 0.16±0.11 thiab 0.15±0.08 ntawm 24, 48, thiab 72 h, ntsig txog. Txawm hais tias cov qhab nia nce me ntsis, optimized ME tsis tshwm sim ua rau tawv nqaij. Vim li no, PG(Phenylethanoild glycoside los ntawm cistanche)kho nrog optimized ME zoo li muaj kev nyab xeeb. Ib qho tshiab ME tau npaj siv IPM ua cov roj theem, CremophorEL ua cov surfactant, thiab propylene glycol ua cov cosurfactant. Qhov no formulation yog yus muaj los ntawm ib tug pob tshab tsos, tsis tshua muaj viscosity, ib tug spherically uniform tis, ruaj khov lub cev thiab tshuaj zog, thiab zoo stability. Piv nrog rau cov kua ntsev, ib qho a1.68-fold nce tau sau tseg hauv daim tawv nqaij permeation tus nqi ntawm PG(Phenylethanoild glycoside los ntawm cistanche)rau optimized microemulsion. Qhov sib npaug ntawm PG hauv microemulsion (4149.650± 37.3 µg·cm-2 ) tau ntau dua li ntawm PG hauv cov kua ntsev (2288.63 ± 20.9 µg· cm -2 ). Tsis tas li ntawd, cov permeability coefficient qhia tau hais tias optimized microemulsion yog ib tug ntau npaum cov cab kuj rau transdermal tus me nyuam ntawm PG tshaj li cov kev daws teeb meem (8.87 ± 0.49 cm / hx{14}} vs. 5.41± 0.12 cm / hx 10-3 ), daim tawv nqaij permeation peev xwm ntawm PG(Phenylethanoild glycoside los ntawm cistanche)tau nce ntxiv los ntawm ME no, uas tej zaum yuav yog vim cov yam ntxwv tshwj xeeb ntawm MEs.

CISTANCHE BENEFIT

Cov ntaub ntawv

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    CISTANCHE BENEFIT


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