Development of solid dispersion formulation containing curcumin and curcuminoids of standardized extract to improve curcumin dissolution and relative bioavailability

Dewi Setyaningsih

Onderzoeksoutput

Samenvatting

Curcumin/curcuminoids is the active compound of Curcuma longa L with superior antioxidant and anti-inflammatory activities. However, clinical application of this compound is limited due to its low bioavailability following oral administration. Solid dispersions have been used to improve solubility and
bioavailability of several lipophilic compounds. This study was aimed at developing a suitable solid dispersion system for the improvement of curcumin dissolution and curcumin bioavailability.
The study was initiated by preparation of solid dispersion of curcumin with several carriers (mannitol, PVP K30, and inulin DP23) using 2 different methods including spray drying (SD), and spray freeze drying (SFD).
The solid dispersion products were characterized by DSC, XRPD, SEM and dissolution behavior.The second step was the preparation of curcuminoids solid dispersions with PVP using SD and vacuum drying methods (VD). DSC, XRPD, SEM, FTIR and dissolution behavior were carried out to evaluate their solid state characteristics. An in vivo study (rats) was carried out to evaluate whether dissolution enhancement as observed in vitro resulted in an improved bioavalaibility.
From the initial study, high dissolution rate of curcumin was obtained from 1) spray dried curcumin-mannitol; 2) spray (freeze) dried solid dispersions of curcumin-PVP K30. Investigation on the molecular embedment of the solid dispersions demonstrated the formation of a nanocrystalline curcumin-mannitol and amorphous state of curcumin-PVP K30 prepared by spray (freeze) drying.
From the curcuminoids solid dispersions, dissolution enhancements were obtained using spray and vacuum drying with formation of amorphous state. However, higher dissolution rate of curcumin was obtained in spray dried curcuminoid-PVP K30. Solid dispersions of curcumin-mannitol (SD CUR-Man) and solid dispersion of curcuminoid prepared by spray drying (SD Ex-PVP K30) were used in the in vivo study. The in vivo study demonstrated bioavailability relative of 105% and more than 2080% for SD CUR-Man and SD Ex-PVP K30, respectively.
Originele taal-2English
KwalificatieDoctor of Philosophy
Toekennende instantie
  • Gadjah Mada University
Begeleider(s)/adviseur
  • Fudholi, A., Supervisor, Externe Persoon
  • Hertiani, T., Co-supervisor, Externe Persoon
  • Hinrichs, Wouter, Co-supervisor
Datum van toekenning3-feb-2016
Plaats van publicatie[Yogyakarta]
Uitgever
StatusPublished - 3-feb-2016
Extern gepubliceerdJa

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