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A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.

Kaur H, Kaur G - J Pharm (Cairo) (2014)

Bottom Line: Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols.Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability.This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.

ABSTRACT
Polyphenols constitute a family of natural substances distributed widely in plant kingdom. These are produced as secondary metabolites by plants and so far 8000 representatives of this family have been identified. Recently, there is an increased interest in the polyphenols because of the evidence of their role in prevention of degenerative diseases such as neurodegenerative diseases, cancer, and cardiovascular diseases. Although a large number of drugs are available in the market for treatment of these diseases, however, the emphasis these days is on the exploitation of natural principles derived from plants. Most polyphenols show low in vivo bioavailability thus limiting their application for oral drug delivery. This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins. Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability. This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

No MeSH data available.


Related in: MedlinePlus

Formulation of curcumin solid dispersions [94].
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590825&req=5

fig6: Formulation of curcumin solid dispersions [94].

Mentions: Nanocrystal Solid Dispersions of Curcumin. Solid dispersions have also been demonstrated to increase the bioavailability of poorly water soluble drugs. Onoue et al. [94] have reported the formulation of solid dispersions of curcumin to enhance its solubility. Three types of curcumin dispersions were formulated, namely, nanocrystal solid dispersion (CSD), amorphous solid dispersion (ASD), and nanoemulsion (NE). Figure 6 shows the schematic representation of preparation of three types of solid dispersions. Diffraction pattern of CSD-curcumin was identical with crystalline curcumin indicating high crystallinity of curcumin whereas ASD-curcumin was found to be amorphous. Release rates of amorphous solid dispersion, nanocrystal solid dispersion, and nanoemulsion formulation were found to be 95% (180 min), 80% (180 min), and 93% (60 min), respectively, thus, indicating enhanced solubility of curcumin with solid dispersions.


A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.

Kaur H, Kaur G - J Pharm (Cairo) (2014)

Formulation of curcumin solid dispersions [94].
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590825&req=5

fig6: Formulation of curcumin solid dispersions [94].
Mentions: Nanocrystal Solid Dispersions of Curcumin. Solid dispersions have also been demonstrated to increase the bioavailability of poorly water soluble drugs. Onoue et al. [94] have reported the formulation of solid dispersions of curcumin to enhance its solubility. Three types of curcumin dispersions were formulated, namely, nanocrystal solid dispersion (CSD), amorphous solid dispersion (ASD), and nanoemulsion (NE). Figure 6 shows the schematic representation of preparation of three types of solid dispersions. Diffraction pattern of CSD-curcumin was identical with crystalline curcumin indicating high crystallinity of curcumin whereas ASD-curcumin was found to be amorphous. Release rates of amorphous solid dispersion, nanocrystal solid dispersion, and nanoemulsion formulation were found to be 95% (180 min), 80% (180 min), and 93% (60 min), respectively, thus, indicating enhanced solubility of curcumin with solid dispersions.

Bottom Line: Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols.Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability.This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.

ABSTRACT
Polyphenols constitute a family of natural substances distributed widely in plant kingdom. These are produced as secondary metabolites by plants and so far 8000 representatives of this family have been identified. Recently, there is an increased interest in the polyphenols because of the evidence of their role in prevention of degenerative diseases such as neurodegenerative diseases, cancer, and cardiovascular diseases. Although a large number of drugs are available in the market for treatment of these diseases, however, the emphasis these days is on the exploitation of natural principles derived from plants. Most polyphenols show low in vivo bioavailability thus limiting their application for oral drug delivery. This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins. Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability. This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

No MeSH data available.


Related in: MedlinePlus