Development and characterization of modern pharmaceutical forms with biochanin A and biological activities

[I. Lj. Gajić]

179, 3 lista

Biografija autora: list 169 Bibliografija: list. 170-179

Chemistry and chemical technology

Biochanin A (BHA) is an O-methylated isoflavone whose chemical structure is 5,7-dihydroxy-3-(4-methoxyphenyl)-chromen-4-one. It is similar to estrogen, so it exhibits agonistic and antagonistic interaction with estrogen receptors. BHA exhibits antioxidant, anti-inflammatory, anti-diabetic, anti-allergic, anti-hyperglycemic, anti-hyperlipidemic and anti-cancer activity. Despite a large number of beneficial effects, its clinical use is limited due to its low solubility in water and poor bioavailability. The inclusion complex of BHA with 2-hydroxypropyl-β-cyclodextrin was prepared by the coprecipitation method and characterized by various instrumental methods which indicate the achieved inclusion of BHA in the cavities of cyclodextrin. Due to the increased solubility in water, the BHA:HP-β-CD inclusion complex exhibited better cholinesterase inhibitory 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 polymerization of NiPAm monomer with 5 mol% AA using 1.5 mol% EGDM as crosslinker. BHA was incorporated into the lyophilized and nonlyophilized copolymer. The effect of pH and temperature on the release rate of BHA from the copolymer was investigated. It was shown that the pH- and thermosensitive copolymer p(NiPAm-co-AA) can be suitable as a carrier for the modified release of BHA in acidic and slightly alkaline environments. Using the electrospinning technique, polymer fibers from PLA and PVP with 2% and 5% BHA were made at room temperature. It was shown that the morphology of the fibers was not changed with the addition of BHA, that it was fully incorporated and that there was no interaction of BHA with the polymer matrices. The release of BHA from PLA electrospun fibers was prolonged, whereas it was rapid and complete from PVP fibers. The influence of electrospun PLA and PVP fibers with and without BHA on L929 fibroblast cell proliferation and wound healing was investigated. MLV liposomes with BHA were obtained using the thin film method, while SUV liposomes of appropriate size and with a narrow size distribution and satisfactory stability were obtained by extrusion. The release of BHA from liposomes was monitored using the dialysis bag technique against a buffer solution.

Biohanin A, inkluzioni kompleks, 2-hidroksipropil--ciklodekstrin, hidrogel, elektrospinovana vlakna, liposomi

Biochanin A, inclusion complex, 2-hydroxypropyl-β-cyclodextrin, hydrogel, electrospun fibers, liposomes

615.01:615.322+577.175.5(043.3)

klasifikacija: T 410

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