Razvoj i karakterizacija savremenih farmaceutskih oblika sa biohaninom A i biološke aktivnosti
Stanojević, Ljiljana, 1976-
Nikolić, Goran S., 1966-
Najman, Stevo, 1955-
Mihajlov-Krstev, Tatjana M., 1988
Dinić, Ana
Biochanin A (BHA) is an O-methylated isoflavone whose chemicalstructure is 5,7-dihydroxy-3-(4-methoxyphenyl)-chromen-4-one. It issimilar to estrogen, so it exhibits agonistic and antagonistic interactionwith estrogen receptors. BHA exhibits antioxidant, anti-inflammatory,anti-diabetic, anti-allergic, anti-hyperglycemic, anti-hyperlipidemic andanti-cancer activity. Despite a large number of beneficial effects, itsclinical use is limited due to its low solubility in water and poorbioavailability.The inclusion complex of BHA with 2-hydroxypropyl-β-cyclodextrin wasprepared by the coprecipitation method and characterized by variousinstrumental methods which indicate the achieved inclusion of BHA in thecavities of cyclodextrin. Due to the increased solubility in water, theBHA:HP-β-CD inclusion complex exhibited better cholinesteraseinhibitory activity and increased antimicrobial and antioxidant activity.The same or better inhibitory effect of BHA was observed on tyrosinase,α-amylase and α-glucosidase.Copolymer p(NiPAm-co-AA) was synthesized by radical polymerizationof NiPAm monomer with 5 mol% AA using 1.5 mol% EGDM ascrosslinker. BHA was incorporated into the lyophilized and nonlyophilizedcopolymer. The effect of pH and temperature on the releaserate of BHA from the copolymer was investigated. It was shown that thepH- and thermosensitive copolymer p(NiPAm-co-AA) can be suitable as acarrier for the modified release of BHA in acidic and slightly alkalineenvironments.Using the electrospinning technique, polymer fibers from PLA and PVPwith 2% and 5% BHA were made at room temperature. It was shown thatthe morphology of the fibers was not changed with the addition of BHA,that it was fully incorporated and that there was no interaction of BHAwith the polymer matrices. The release of BHA from PLA electrospunfibers was prolonged, whereas it was rapid and complete from PVPfibers. The influence of electrospun PLA and PVP fibers with and withoutBHA on L929 fibroblast cell proliferation and wound healing wasinvestigated.MLV liposomes with BHA were obtained using the thin film method,while SUV liposomes of appropriate size and with a narrow sizedistribution and satisfactory stability were obtained by extrusion. Therelease of BHA from liposomes was monitored using the dialysis bagtechnique against a buffer solution.
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Serbian
2024
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