Complex Coacervated Microcapsules In Cream For Topical Delivery Of The Curcuminoids And Quercetin
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Date
2015-12
Authors
Ang, Lee Fung
Journal Title
Journal ISSN
Volume Title
Publisher
Universiti Sains Malaysia
Abstract
The curcuminoids and quercetin possess antioxidant, anti-inflammatory and
antibacterial activities which are beneficial for wound healing. However, poor
solubility, poor bioavailability, photosensitivity and color staining properties of these
two compounds make them not acceptable for topical administrations. Therefore, the
objectives of the present study were to develop and characterize the
curcuminoids/quercetin microcapsules and subsequently incorporate them in cream.
Isocratic reversed phase UV HPLC was developed and validated to quantify the
curcuminoids (bisdemethoxycurcumin, demethoxycurcumin and curcumin) and
quercetin simultaneously. The peaks of quercetin, bisdemethoxycurcumin,
demethoxycurcumin and curcumin were well separated and symmetrical. The
microcapsules were prepared by complex coacervation method using chitosan and
gelatin B. The best microcapsules were obtained at gelatin:chitosan ratio of 30:1
(2.55% w/w) and pH 5.50. The curcuminoids was encapsulated either in liquid
(CLM) or solid (CPM) form. The quercetin was also encapsulated either in liquid
(QLM) or solid (QPM) form. The physical characteristics of CPM and QPM were
better than CLM and QLM. The CPM and QPM had particle size in the range of 40 –
44 μm, entrapment efficiency of 82% and drug loading of 16%. Moreover, the
microcapsules had free flowing, reduce color staining effect and stable at room
temperature (28 °C) for 12 months. The antioxidant activity of the curcuminoids and
quercetin was higher than butylated hydroxyanisole (BHA) and butylated
hydroxytoluene (BHT). There was no significant change in antioxidant activity of the
curcuminoids and quercetin after encapsulation in microcapsules. The curcuminoids
and quercetin microcapsules were then incorporated in O/W cream base,
respectively. The preparations had pseudoplastic and thixotropic properties. In vitro
release study revealed that the curcuminoids and quercetin released from
microcapsule incorporated in cream followed zero order kinetics. The CPM and
QPM creams were stable at room temperature (28 °C) for 6 months. The skin
irritation test in rabbit revealed that both preparations were nonirritant. Furthermore,
the in vivo wound healing study in rats showed that CPM and QPM creams had
wound healing properties. In conclusion, the curcuminoids and quercetin
microcapsules incorporated in creams were successfully prepared. CPM had better
wound healing property than QPM.
Description
Keywords
Curcuminoids and quercetin