Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy
Curcumin, a functional food polyphenol reported to inhibit cancer cell proliferation, invasion, angiogenesis and metastasis through interaction with multiple molecular targets. However, the clinical usefulness of curcumin in the treatment of cancer is limited due to poor solubility in water at acidi...
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Tsinghua University Press
2014-06-01
|
| Series: | Nano Biomedicine and Engineering |
| Subjects: | |
| Online Access: | https://www.sciopen.com/article/10.5101/nbe.v6i2.p47-59 |
| _version_ | 1797673438040555520 |
|---|---|
| author | Moorthi Chidambaram Kathiresan Krishnasamy |
| author_facet | Moorthi Chidambaram Kathiresan Krishnasamy |
| author_sort | Moorthi Chidambaram |
| collection | DOAJ |
| description | Curcumin, a functional food polyphenol reported to inhibit cancer cell proliferation, invasion, angiogenesis and metastasis through interaction with multiple molecular targets. However, the clinical usefulness of curcumin in the treatment of cancer is limited due to poor solubility in water at acidic and neutral pH, hydrolytic degradation in alkaline pH and metabolism in the liver and intestine, resulting in decreased or absence of therapeutic efficacy. Hence, the present study was aimed to overcome the limitations of curcumin in the treatment of cancer by codelivery of nanosized curcumin and bioenhancer using acid degradable polymeric nanoparticles. Modified nanoprecipitation method was used to prepare void, curcumin-piperine, curcumin-quercetin and curcumin-silibinin encapsulated polymeric nanoparticles. Prepared nanoformulations were evaluated for particle size, polydispersity index, zeta potential, surface morphology, drug content, encapsulation efficiency, drug loading, in vitro release, stability at elevated storage conditions, toxicity on normal liver cells, anticancer activity on various cancer cell lines and on cancer induced rats. Prepared curcumin-bioenhancer encapsulated polymeric nanoparticles were (a) spherical in shape with size <100 nm and displayed excellent uniformity; (b) showed >95% release of curcumin and bioenhancers within 45 minutes in gastric fluid; (c) proved non-toxic to normal liver cells; (d) extremely stable at elevated storage conditions; and (e) demonstrated enhanced anticancer activity against various cancer cell lines and mammary cancer in rats than the pure curcumin. Study concludes that the prepared curcumin-bioenhancer encapsulated polymeric nanoformulations significantly overcome the limitations of curcumin in the treatment of cancer and synergistically enhance its anticancer activity. However, out of three polymeric nanoformulations, curcumin-silibinin polymeric nanoformulation showed superior anticancer activity. |
| first_indexed | 2024-03-11T21:45:30Z |
| format | Article |
| id | doaj.art-592e6caf92bf43f781b26bd1560e3a07 |
| institution | Directory Open Access Journal |
| issn | 2150-5578 |
| language | English |
| last_indexed | 2024-03-11T21:45:30Z |
| publishDate | 2014-06-01 |
| publisher | Tsinghua University Press |
| record_format | Article |
| series | Nano Biomedicine and Engineering |
| spelling | doaj.art-592e6caf92bf43f781b26bd1560e3a072023-09-26T10:12:56ZengTsinghua University PressNano Biomedicine and Engineering2150-55782014-06-0162475910.5101/nbe.v6i2.p47-59Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer EfficacyMoorthi Chidambaram0Kathiresan Krishnasamy1Department of Pharmacy, Annamalai University, Annamalai Nagar - 608 002, Chidambaram, Tamil Nadu, IndiaDepartment of Pharmacy, Annamalai University, Annamalai Nagar - 608 002, Chidambaram, Tamil Nadu, IndiaCurcumin, a functional food polyphenol reported to inhibit cancer cell proliferation, invasion, angiogenesis and metastasis through interaction with multiple molecular targets. However, the clinical usefulness of curcumin in the treatment of cancer is limited due to poor solubility in water at acidic and neutral pH, hydrolytic degradation in alkaline pH and metabolism in the liver and intestine, resulting in decreased or absence of therapeutic efficacy. Hence, the present study was aimed to overcome the limitations of curcumin in the treatment of cancer by codelivery of nanosized curcumin and bioenhancer using acid degradable polymeric nanoparticles. Modified nanoprecipitation method was used to prepare void, curcumin-piperine, curcumin-quercetin and curcumin-silibinin encapsulated polymeric nanoparticles. Prepared nanoformulations were evaluated for particle size, polydispersity index, zeta potential, surface morphology, drug content, encapsulation efficiency, drug loading, in vitro release, stability at elevated storage conditions, toxicity on normal liver cells, anticancer activity on various cancer cell lines and on cancer induced rats. Prepared curcumin-bioenhancer encapsulated polymeric nanoparticles were (a) spherical in shape with size <100 nm and displayed excellent uniformity; (b) showed >95% release of curcumin and bioenhancers within 45 minutes in gastric fluid; (c) proved non-toxic to normal liver cells; (d) extremely stable at elevated storage conditions; and (e) demonstrated enhanced anticancer activity against various cancer cell lines and mammary cancer in rats than the pure curcumin. Study concludes that the prepared curcumin-bioenhancer encapsulated polymeric nanoformulations significantly overcome the limitations of curcumin in the treatment of cancer and synergistically enhance its anticancer activity. However, out of three polymeric nanoformulations, curcumin-silibinin polymeric nanoformulation showed superior anticancer activity.https://www.sciopen.com/article/10.5101/nbe.v6i2.p47-59curcuminpiperinepolymeric nanoparticlequercetinsilibinin |
| spellingShingle | Moorthi Chidambaram Kathiresan Krishnasamy Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy Nano Biomedicine and Engineering curcumin piperine polymeric nanoparticle quercetin silibinin |
| title | Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy |
| title_full | Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy |
| title_fullStr | Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy |
| title_full_unstemmed | Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy |
| title_short | Codelivery of Nanosized Curcumin and Bioenhancer using Acid Degradable Polymeric Nanoparticles Displayed Enhanced Anticancer Efficacy |
| title_sort | codelivery of nanosized curcumin and bioenhancer using acid degradable polymeric nanoparticles displayed enhanced anticancer efficacy |
| topic | curcumin piperine polymeric nanoparticle quercetin silibinin |
| url | https://www.sciopen.com/article/10.5101/nbe.v6i2.p47-59 |
| work_keys_str_mv | AT moorthichidambaram codeliveryofnanosizedcurcuminandbioenhancerusingaciddegradablepolymericnanoparticlesdisplayedenhancedanticancerefficacy AT kathiresankrishnasamy codeliveryofnanosizedcurcuminandbioenhancerusingaciddegradablepolymericnanoparticlesdisplayedenhancedanticancerefficacy |