Kungani i-Silymarin Ine-Bioavailability Ephansi—nokuthi Ukulethwa Kwe-Liposomal Kuthuthukisa Kanjani Ukumuncwa

Kososayensi bokwakha, abaqondisi be-R&D, kanye nabanikazi bomkhiqizo abathuthukisa{0}}isizukulwane esilandelayo imikhiqizo yezempilo yesibindi, ukuqonda indlela yokwenzaliposomal silymarinkubalulekile ekukhetheni isithako unolwazi kanye nokuma komkhiqizo. I-Silymarin{1}}i-bioactive flavonolignan complex evela ku-milk thistle (I-Silybum marianum){0}}iqashelwa kabanzi nge-hepatoprotective, antioxidant, kanye{1}nezici zayo zokuqeda ukuvuvukala. Kodwa-ke, izingcaphuno ze-silymarin ezivamile ziye zabhekana nomkhawulo obalulekile ngokungaguquki: inhlanganisela ibonisa ukuncibilika okungalungile kwe-aqueous, ukumuncwa okulinganiselwe kwamathumbu, kanye{3}}nomzimba omningi wokuqala wokudlula, okuholela ekungabiniki kahle komlomo kwe-bioavailability. Ukugxila okusebenzayo kwe-flavonolignans ku-plasma kubikwe ebangeni lama-50 kuye kwangama-300 ng/mL, nge-Tmax cishe yamahora angu-6–8, okubonisa ukuchayeka okulinganiselwe kwesistimu okuhlobene nokubunjwa okujwayelekile kwe-silymarin. Nakuba ukumuncwa komlomo okubikiwe kwe-silymarin cishe kungama-23%–47%, okubanzi{12}}okudlula i-metabolism kukhawulela nakakhulu ukuchayeka kwesistimu.I-Liposomal silymarin powderibhekana nalezi zinselele ngokusebenzisa i-phospholipid encapsulation, enikeza indlela yokulethwa eklanyelwe ukuthuthukisa ukuhlakazeka nokutholakala kwesistimu kwalesi sakhi esibalulekile se-bioactive.

 

 

 

Ukungatholakali kahle kwe-oral bioavailability ye-Silymarin ku-multifactorial, okuvela ezithiyo ezintathu eziyinhloko.

Isithiyo 1: Ukunyibilika Okunamanzi Okuphansi

I-Silymarin iyinhlanganisela ye-hydrophobic ene-solubility ephansi kakhulu yamanzi. Ukuncibilika kwamanzi kubikwa ngaphansi kuka-50 ug/mL, okukhawulela kakhulu ukuhlakazeka emgudwini wamathumbu. Imvelo ye-lipophilic yalawa ma-flavonolignans iholela ekuncibilikeni okuphansi emanzini, futhi uma isimunnyiwe, i-metabolism ebanzi yokuqala{3}}yedlula iphinde yehlise ukusebenza kahle kwayo kokwelapha lapho isetshenziswa ngendlela evamile.

Isithiyo sesi-2: Ukungena Amathumbu Okukhawulelwe

I-Silymarin flavonolignans ikhombisa ukungeneka kwamathumbu okulinganiselwe, kuyilapho izithuthi ze-efflux ezifana ne-MRP2 ne-BCRP zingase zibeke imingcele ukumuncwa kwesistimu. I-coefficient ebonakalayo yokungena iphansi, ikhawulela inani lenhlanganisela esebenzayo etholakalayo yokumuncwa kwesistimu. Ukumuncwa kabi kwamathumbu, ukuqina kwe-metabolism esibindini, kanye nokuphuma ngokushesha kwe-silymarin kunciphisa ukugcwala kwe-silymarin ekujikelezeni kwegazi futhi ngenxa yalokho endaweni okuhlosiwe.

Isithiyo 3: I-Metabolism Ebanzi Yokuqala-Yokudlula

Uma isimuncwe, i-silymarin ingena ngokushesha futhi idlulele{0}idlule i-metabolism, ngokuyinhloko emathunjini nasesibindini. Ukususwa kwe-silymarin kuhilela{2}}i-pass metabolism enkulu kakhulu, okuyinto ikakhulukazi ngokuhlangana kwesigaba II. Le nqubo yemetabolism iqondiswa ngokuyinhloko yi-UDP-glucuronosyltransferase (UGT) isoforms (ikakhulukazi i-UGT1A1, 1A6, 1A7, 1A9, 2B7, kanye ne-2B15). I-Silymarin flavonolignans ibhekana ngokushesha{18}nokuqala nokudlula imetabolism ngokuyinhloko nge-glucuronidation. Ucwaningo lwe-pharmacokinetic yabantu lubonise ukuthi i-glucuronidated ne-sulfated conjugates yenza izinhlobo ezinkulu ezijikelezayo ze-silymarin flavonolignans, cishe ngama-55% nama-28%, ngokulandelana, abonwa eduze nokugxila okuphezulu kwe-plasma.

Izinhlanganisela zomzali nama-conjugates azo nazo zingaphansi kokuphuma kwe-efflux ku-lumen yamathumbu ngabathuthi abafana ne-MRP2 ne-BCRP, okuqhubeka nokukhawulela ukumuncwa kwesistimu. Ngaphansi kuka-3% womthamo olawulwayo ukhishwa emchamweni njengomuthi ongashintshiwe.

Umthelela Oqongelelekayo

Umthelela onqwabelene walezi zithiyo ukuthi imikhiqizo ye-silymarin evamile iletha ingxenye encane kuphela yokuqukethwe kwayo okunelebula ekujikelezeni kwesistimu. Nakuba ukumuncwa kwe-silymarin emathunjini kuye kwabikwa ebangeni elicishe libe ngu-23%–47%, okubanzi{3}}okudlula i-metabolism kanye nokuqeda ngokushesha kungakhawulela kakhulu ukuvezwa kwesistimu kwama-flavonolignans aqinile.

 

 

Ubuchwepheshe bokulethwa kwe-Liposomal bubhekana nezinselelo ze-bioavailability ze-silymarin ngokusebenzisa i-phospholipid encapsulation. Ama-molecule e-Silymarin ahlanganiswe ngaphakathi kwama-bilayers e-phospholipid{1}}ngokuvamile atholakala{2}}ku-GMO sunflower phosphatidylcholine{3}okwakha ama-nanoscale vesicles anezinhlayiyana ezilawulwayo nezifanayo{4}}nokusabalalisa usayizi.

I-Solubilisation Ethuthukisiwe Nokusabalalisa

I-encapsulation iguqula i-silymarin enganyibiliki kahle ibe ifomu elingasatshalaliswa endaweni enamanzi. Lokhu kubhekana nesithiyo esiyinhloko sokuncibilika okune-aqueous okuphansi, okuvumela ukuncibilika okungaguquki emgudwini wamathumbu. Ucwaningo lubonise ukuthi i-silymarin{2}}ama-liposome alayishiwe nama-polymeric micelles athuthukisa i-bioavailability kanye nempumelelo yokwelapha.

Ukuguqulwa Kokuziphatha Kwamathumbu

I-phospholipid bilayer ingashintsha ukuziphatha kwamathumbu e-silymarin futhi ingase isize ukuthuthukisa ukuhlakazeka kwayo futhi ivikele inhlanganisela ehlanganisiwe ngaphansi kwezimo ezithile zokubunjwa. Ama-liposomes avamile abonise i-bioavailability ethuthukisiwe uma kuqhathaniswa ne-silymarin iyodwa. Ama-Liposomes atholwe kuma-phospholipids emvelo ahambisana ne-biocompatible futhi ayabola, futhi angahlanganisa inhlobonhlobo yezidakamizwa ezincibilika emanzini kanye ne-lipid.

I-Lymphatic Transport engaba khona kanye nokusebenzisana kwamaselula

Amasistimu athile okulethwa e-lipid-angase enze lula ukuthuthwa kwe-lymphatic futhi aguqule ukumuncwa kanye nokusetshenziswa kwezinhlanganisela ezinganyibiliki kahle. Amasistimu we-Liposomal angasebenzisana nolwelwesi lwamathumbu futhi angashintsha ukukhululwa, ukuthutha, kanye nokuthathwa kwamaselula kwamakhompiyutha ahlanganisiwe.

 

 

Ubufakazi Be-Preclinical be-Liposomal Silymarin

Ucwaningo olushicilelwe kuImibiko Yemithi(2014) ithuthukise isistimu yenethiwekhi ye-lecithin{1}esekelwe ku-silymarin ehlanganisa indlela ye-phytosomal{2}}liposomal. Ukwakheka kwe-liposomal kuveze ai-bioavailability ephezulu ephindwe kathathu nesigamuwe-silymarin uma kuqhathaniswa nokumiswa kwe-silymarin lapho kuhlolwa kumagundane e-Wistar. Ukwakheka kubonise ukungena okuphezulu okungama-55% kwesilinganiso se-lecithin-cholesterol esingu-6:1, futhi kwabonisa ukusebenza kahle kwe-hepatoprotection okungcono (isikhathi esisodwa nesigamu) kanye nokuvimbela okungcono kokukhiqizwa kwezinhlobo zomoya-mpilo osebenzayo (izikhathi eziyishumi) uma kuqhathaniswa ne-silymarin. Kumamodeli we-vivo, ukubunjwa kutholakale kuphumelela kakhulu kunokumiswa kwe-silymarin ekuvikeleni isibindi ngokumelene nobuthi kanye nezimo ezihambisanayo zokuvuvukala.

Ucwaningo olushicilelwe kuIjenali yeKhemistry Yezolimo Nezokudla(I-2014) ilungiselele ukwakheka kwe-silymarin okufakwe ku-liposomes kanye ne-ethosomes (i-LSM ne-ESM, ngokulandelana) ukuze kuthuthukiswe i-bioavailability yomlomo nokuhlola ukusatshalaliswa kwezicubu. Imiphumela ibonise ukuthi ukwakheka kwe-liposomal kanye ne-ethosomal encapsulated ye-silymarin kungase kunikeze ukusatshalaliswa kwezicubu okuphumelelayo kanye nokwanda kwe-bioavailability yomlomo, ngaleyo ndlela kuthuthukise izakhiwo zayo zokwelapha emzimbeni.

Ucwaningo olwengeziwe lwe-Liposomal Silymarin

Ucwaningo lwama-liposomes alayishiwe e-silymarin-aqukethe usawoti wenyongo olungiselelwe ubuchwepheshe boketshezi olunamandla kakhulu lubike ukwakheka okulungiselelwe okunosayizi wezinhlayiyana ongu-160.5 nm, ukusebenza kahle kwe-entrapment okungu-91.4%, kanye ne-vivo AUC₀₋ₜ4.8-okungaphezulukunaleyo ye-silymarin powder.

Le miphumela iyakhiwa{0}}iqondile futhi akufanele ihunyushwe njengezilinganiso zokusebenza kwendawo yonke yayo yonke imikhiqizo ye-liposomal silymarin. I-bioavailability yezentengiselwano kufanele isungulwe ngomkhiqizo{2}}ucwaningo oluthile lwe-pharmacokinetic.

 

 

Kubathengi be-B2B,i-liposomal silymarin powderinikeza izinzuzo ezifanele zezentengiso ezidlulela ngale kwamamethrikhi e-pharmacokinetic.

Umehluko Womkhiqizo

Emakethe yezempilo yesibindi eminyene, i-bioavailability iyindawo ekhonjiswayo yokuhlukanisa. Idatha ye-Pharmacokinetic inganikeza isisekelo esengeziwe sokuhlukaniswa komkhiqizo lapho ukwakheka{1}}kutholakala ubufakazi obuqondile. Lokhu kubaluleke kakhulu emikhiqizweni{3}ebekwe endaweni ephambili eqondise ezempilo{4}}abathengi abanolwazi abafuna ukwakheka{5}}okusekelwe isayensi.

Ukuvumelana nezimo

I-Liposomal silymarin itholakala ngamafomethi amaningi ukuze ihlangabezane nezidingo-zomkhiqizo oqediwe ohlukahlukene:

Ifomethi	Izici	Izinhlelo zokusebenza
Friza-impushana ye-liposomal eyomisiwe	Izinzile, kulula ukuyifaka	Amaphilisi, amaphilisi, amaphakethe wenduku
Fafaza-impushana ye-liposomal eyomisiwe	Izakhiwo ezinhle zokugeleza	Ama-Blends, ama-sachets
Ukumiswa kwe-liposomal ye-Liquid	Ulungele-ukusetshenziswa{1}}	Iziphuzo, izithasiselo eziwuketshezi

Abahlinzeki banikeza ukugxila okuhlukahlukene ukuze kuhlangatshezwane nezidingo ezithile zokwakheka.

Amandla Okwenza Idosi

I-bioavailability ethuthukisiwe ingase idale amathuba okuhlola ukuthuthukiswa komthamo ngesikhathi sokuthuthukiswa kokwakhiwa, nakuba noma yikuphi ukuncipha komthamo wesithako esisebenzayo kufanele kusekelwe idatha yomkhiqizo{0}}yekhemisi ethile kanye nokusebenza ngempumelelo.

Ukwethembeka Kochungechunge Lokuthenga

Kochwepheshe bokuthenga, ukucatshangelwa okubalulekile kudlulela ngale kwesithako ngokwaso:

• Ukukhiqiza okuhlanganisiwe okuqondileiqinisekisa inqwaba-kuya{1}}ukuvumelana kwenqwaba
• Izitifiketi eziphelele(cGMP, ISO 22000, FSSC 22000, HACCP) inikeza isiqiniseko esilawulayo sokufinyelela ezimakethe zomhlaba
• Ukusekelwa kwamadokhumenti(i-COA, i-TDS, i-SDS, idatha yokuzinza, ukuhlaziya usayizi wezinhlayiyana) kuqondisa ukuqinisekiswa kwekhwalithi nokuthobela imithetho

 

 

 

Ukushintsha ukusuka kwejwayelekile ukuya ku-liposomal silymarin akukhona nje ukuthuthukiswa kokwakheka{0}}kuyisinqumo esinamasu esinemithelela ekusebenzeni komkhiqizo, ukuma kwebhrendi, nempumelelo yezohwebo.

Kubakhiqizi{0}abaqedile bomkhiqizo, izinzuzo ezibalulekile yilezi:

• Ukuxhumana okuthembekile kwesayensi: Idatha ye-Pharmacokinetic ingasekela ukuhlukaniswa komkhiqizo kanye nokuxhumana kwezobuchwepheshe namakhasimende e-B2B
• Ukuhlukaniswa komkhiqizo: Ukwakhiwa-idatha ethile ye-pharmacokinetic inganikeza isisekelo esengeziwe sokuma okuhlukile emakethe yesithako ephambili.
• Ukulungela ukulawula: Amaphakheji aphelele amadokhumenti asiza ukungena emakethe ngokushesha ezindaweni eziningi

Kubakhiqizi bezinkontileka-nabahlinzeki belebula abazimele, ukunikeza i-liposomal formulations kwandisa iphothifoliyo yesevisi futhi kubeka inkampani esikhundleni njengomholi wezobuchwepheshe kunokuba umdayisi wesithako sempahla.

 

 

I-silymarin evamile ihlushwa i-bioavailability yesistimu elinganiselwe ngenxa yezithiyo ezintathu ezibalulekile: ukunyibilika okuphansi kwamanzi, ukungeneka okulinganiselwe kwamathumbu, kanye -nomzimba omkhulu wokudlula we-metabolism ngokuyinhloko nge-glucuronidation ne-sulfation. Nakuba ukumuncwa kwe-silymarin emathunjini kuye kwabikwa ebangeni elicishe libe ngu-23%–47%, i-metabolism eningi kanye nokuqedwa kunganciphisa kakhulu ukuchayeka kwesistimu kuma-flavonolignans aphelele. ubuchwepheshe bokulethwa kwe-liposomal bubhekana nale mikhawulo ngokufaka i-silymarin ngaphakathi kwe-phospholipid bilayers engathuthukisa i-solubilisation, iguqule indlela yokuziphatha emathunjini, futhi ibe nomthelela ekukhululweni kanye nokuthathwa kwamaselula kwenhlanganisela ehlanganisiwe. Ucwaningo lwe-preclinical lubonise ukuthuthuka okuphawulekayo kumapharamitha we-pharmacokinetic-okuhlanganisa 3.5-i-bioavailability ephakeme ephindwe ka-3.5-ye-liposomal formulation ethile kumagundane e-Wistar kanye ne-AUC ephindwe izikhathi ezingu-4.8 ephakeme ye-bile salt-containing liposomal formulation.

Le miphumela iyakhiwa{0}}iqondile futhi akufanele ihunyushwe njengezilinganiso zokusebenza kwendawo yonke yayo yonke imikhiqizo ye-liposomal silymarin. Kubathengi be-B2B-abadidiyeli, abaqondisi be-R&D, abaphathi bokuthengwa kwempahla, nabanikazi bomkhiqizo{4}}i-liposomal silymarin ayimeleli nje ukukhetha kokwakhiwa, kodwa ukutshalwa kwezimali kwamasu ekusebenzeni komkhiqizo nokwethembeka komkhiqizo.

 

Ingabe usukulungele ukuhlola i-liposomal silymarin ukuze uthole ukwakheka kwakho okulandelayo?Ithimba lethu lezobuchwepheshe liyatholakala ukuze lixoxisane ngezimfuneko zokucaciswa, linikeze idatha yokuzinza, futhi lisekele ukuthuthukiswa komkhiqizo wakho kusukela kumqondo kuya ekuqalisweni kwezentengiso.

• Cela isampulaokokuhlola{0}kwasendlini kanye nezivivinyo zokwakha
• Landa iphakheji yedatha yobuchwepheshe(COA, izifundo zokuzinza, ukuhlaziywa kosayizi wezinhlayiyana)
• Buza mayelana nokucaciswa ngokwezifiso(ukugxila, usayizi wezinhlayiya, izinketho ze-excipient)
• Hlela ukubonisana kwezobuchwepheshenososayensi bethu bokwakha

[Thinta ithimba lethu le-B2B namuhla ukuze uxoxe ngezimfuneko zakho.]

I-imeyili:liu@wellgreenxa.com

 

 

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5. Xie Y, Miranda SR, Hoskins JM, Hawke RL. Iqhaza le-UDP-I-Glucuronosyltransferase 1A1 ku-Metabolism ne-Pharmacokinetics ye-Silymarin Flavonolignans Ezigulini ezine-HCV ne-NAFLD.Amangqamuzana. 2017;22(1):142. doi:10.3390/molecules22010142