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A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.

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

Bottom Line: This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins.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

APSP and EPN techniques for nanoparticle formulation of curcumin [92].
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590825&req=5

fig5: APSP and EPN techniques for nanoparticle formulation of curcumin [92].

Mentions: It is a naturally occurring polyphenol which is extracted from the plants of Curcuma longa. Curcuma longa (turmeric) has been used to treat ailments since a long time ago. It is also employed as a spice in Indian cuisine. Curcumin exhibits a variety of pharmacological actions such as antitumor [87], anti-HIV [88], antioxidant, and anti-inflammatory [89]. However, the goodness of curcumin has not been able to reach up to its potential yet. The maximum solubility of curcumin in plain aqueous buffer pH 5.0 has been reported to be 11 ng/mL [90] and the oral dose of curcumin for treating advanced colorectal cancer was found to be 3.6 g/day [91]. Therefore, there is need to devise strategies to increase solubility of curcumin. Nanoparticles of curcumin employing antisolvent precipitation method have been reported by Kakran et al. [92]. The antisolvent precipitation involved two methods, namely, antisolvent precipitation using a syringe pump (APSP) and evaporative precipitation of nanosuspension (EPN). In first method ethanol was used as solvent and deionized water as antisolvent. In EPN method solvent was same but antisolvent employed was hexane. Figure 5 depicts a schematic representation of techniques employed for formulation of nanoparticles. The effect of process variables such as stirring speed, flow rate, solvent : antisolvent (S : AS) ratio, and drug concentration was studied on particle size and solubility.


A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.

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

APSP and EPN techniques for nanoparticle formulation of curcumin [92].
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig5: APSP and EPN techniques for nanoparticle formulation of curcumin [92].
Mentions: It is a naturally occurring polyphenol which is extracted from the plants of Curcuma longa. Curcuma longa (turmeric) has been used to treat ailments since a long time ago. It is also employed as a spice in Indian cuisine. Curcumin exhibits a variety of pharmacological actions such as antitumor [87], anti-HIV [88], antioxidant, and anti-inflammatory [89]. However, the goodness of curcumin has not been able to reach up to its potential yet. The maximum solubility of curcumin in plain aqueous buffer pH 5.0 has been reported to be 11 ng/mL [90] and the oral dose of curcumin for treating advanced colorectal cancer was found to be 3.6 g/day [91]. Therefore, there is need to devise strategies to increase solubility of curcumin. Nanoparticles of curcumin employing antisolvent precipitation method have been reported by Kakran et al. [92]. The antisolvent precipitation involved two methods, namely, antisolvent precipitation using a syringe pump (APSP) and evaporative precipitation of nanosuspension (EPN). In first method ethanol was used as solvent and deionized water as antisolvent. In EPN method solvent was same but antisolvent employed was hexane. Figure 5 depicts a schematic representation of techniques employed for formulation of nanoparticles. The effect of process variables such as stirring speed, flow rate, solvent : antisolvent (S : AS) ratio, and drug concentration was studied on particle size and solubility.

Bottom Line: This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins.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