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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

Steps involved in SAS method for preparation of nanoparticles [55].
© Copyright Policy - open-access
Related In: Results  -  Collection


getmorefigures.php?uid=PMC4590825&req=5

fig3: Steps involved in SAS method for preparation of nanoparticles [55].

Mentions: Another method for improvement in solubility of AP has been reported by Zhang et al. [55]. The study incorporated preparation of AP nanocrystals via supercritical antisolvent method (SAS). Figure 3 depicts a schematic representation of preparation of nanoparticles. Photon correlation spectroscopy (PCS) studies revealed the particle size to be 562.5 ± 56 nm with a PI value of 0.92 ± 0.21. Reduced degree of crystallinity was represented in XRPD diagram. Differential scanning calorimetry (DSC) curves of AP coarse powder and AP nanocrystals were studied and compared. A decrease in melting point of AP was observed with nanoparticles which could be attributed to particle size reduction to nanometer range. FTIR patterns were identical for both coarse powder and nanoparticles thus indicating the chemical stability of AP during SAS process. AP nanocrystals exhibited more rapid dissolution rate with much higher cumulative amount of dissolved AP than AP coarse powder. The higher dissolution of AP nanocrystals could be due to the enhanced saturated solubility resulting from a significant decrease of particle size [56]. In vivo studies showed 3.6 and 3.4 fold enhancement in Cmax⁡ and AUC of AP, respectively, after oral administration of AP nanocrystals. The absolute bioavailability of AP coarse powder was found to be 2.0% whereas nanoparticles exhibited 6.9% absolute bioavailability. Thus improved solubility, dissolution rate, and bioavailability depict the usefulness of these methods for delivery of such BCS class second compounds.


A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.

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

Steps involved in SAS method for preparation of nanoparticles [55].
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: Steps involved in SAS method for preparation of nanoparticles [55].
Mentions: Another method for improvement in solubility of AP has been reported by Zhang et al. [55]. The study incorporated preparation of AP nanocrystals via supercritical antisolvent method (SAS). Figure 3 depicts a schematic representation of preparation of nanoparticles. Photon correlation spectroscopy (PCS) studies revealed the particle size to be 562.5 ± 56 nm with a PI value of 0.92 ± 0.21. Reduced degree of crystallinity was represented in XRPD diagram. Differential scanning calorimetry (DSC) curves of AP coarse powder and AP nanocrystals were studied and compared. A decrease in melting point of AP was observed with nanoparticles which could be attributed to particle size reduction to nanometer range. FTIR patterns were identical for both coarse powder and nanoparticles thus indicating the chemical stability of AP during SAS process. AP nanocrystals exhibited more rapid dissolution rate with much higher cumulative amount of dissolved AP than AP coarse powder. The higher dissolution of AP nanocrystals could be due to the enhanced saturated solubility resulting from a significant decrease of particle size [56]. In vivo studies showed 3.6 and 3.4 fold enhancement in Cmax⁡ and AUC of AP, respectively, after oral administration of AP nanocrystals. The absolute bioavailability of AP coarse powder was found to be 2.0% whereas nanoparticles exhibited 6.9% absolute bioavailability. Thus improved solubility, dissolution rate, and bioavailability depict the usefulness of these methods for delivery of such BCS class second compounds.

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