Lipid- and TPGS-Based Core–Shell-Type Nanocapsules Endowed with High Paclitaxel Loading and Enhanced Anticancer Potential
The current study elucidates the improved drug loading of paclitaxel (PTX) in lipid- and d -α-tocopheryl polyethylene glycol succinate (TPGS)–based core–shell-type lipid nanocapsules (PTX-TPGS-LNC) for augmenting the therapeutic efficacy and curbing the toxicity. PTX-TPGS-LNCs were formulated by emp...
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| Veröffentlicht in: | AAPS PharmSciTech 2022-08, Vol.23 (7), p.238-238, Article 238 |
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| creator | Katiyar, Sameer S. Patil, Ravindra Ghadi, Rohan Kuche, Kaushik Kushwah, Varun Dora, Chander Parkash Jain, Sanyog |
| description | The current study elucidates the improved drug loading of paclitaxel (PTX) in lipid- and
d
-α-tocopheryl polyethylene glycol succinate (TPGS)–based core–shell-type lipid nanocapsules (PTX-TPGS-LNC) for augmenting the therapeutic efficacy and curbing the toxicity. PTX-TPGS-LNCs were formulated by employing anti-solvent precipitation technique and displayed a particle size of 162.1 ± 4.70 nm and % practical drug loading of 15.04 ± 2.44%. Electron microscopy revealed that PTX-TPGS-LNCs have spherical morphology and the inner core was surrounded by a relatively lighter region, i.e., layer of lipids and TPGS. The nature of loaded PTX inside the PTX-TPGS-LNC was also confirmed using DSC and PXRD analysis. The
in vitro
release study showed biphasic and sustained release pattern of PTX from PTX-TPGS-LNC and it showed ~ threefold higher PTX uptake in MCF-7 cell line in comparison to free PTX. Moreover, it was apparent from the cytotoxicity assay that PTX-TPGS-LNC displayed higher cytotoxicity in MCF-7 cells and revealed ~ 2.92-fold decrease in IC
50
value as against free PTX when incubated for 72 h. The apoptotic index in case of PTX-TPGS-LNC was ~ twofold higher than free PTX. The pharmacokinetic profile of PTX-TPGS-LNC revealed a ~ 3.18-fold increase in
t
1/2
and a ~ 2.62-fold higher AUC
(0→∞)
compared to Intaxel
®
. Finally, treatment with PTX-TPGS-LNC demonstrated significant lowering in the % tumor burden and serum toxicity markers compared to marketed formulation Intaxel
®
. Thus, the lipid- and TPGS-based core–shell-type LNC with high PTX loading can advance the existing standards of therapy for overshadowing cancer.
Graphical abstract |
| doi_str_mv | 10.1208/s12249-022-02389-4 |
| format | Article |
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d
-α-tocopheryl polyethylene glycol succinate (TPGS)–based core–shell-type lipid nanocapsules (PTX-TPGS-LNC) for augmenting the therapeutic efficacy and curbing the toxicity. PTX-TPGS-LNCs were formulated by employing anti-solvent precipitation technique and displayed a particle size of 162.1 ± 4.70 nm and % practical drug loading of 15.04 ± 2.44%. Electron microscopy revealed that PTX-TPGS-LNCs have spherical morphology and the inner core was surrounded by a relatively lighter region, i.e., layer of lipids and TPGS. The nature of loaded PTX inside the PTX-TPGS-LNC was also confirmed using DSC and PXRD analysis. The
in vitro
release study showed biphasic and sustained release pattern of PTX from PTX-TPGS-LNC and it showed ~ threefold higher PTX uptake in MCF-7 cell line in comparison to free PTX. Moreover, it was apparent from the cytotoxicity assay that PTX-TPGS-LNC displayed higher cytotoxicity in MCF-7 cells and revealed ~ 2.92-fold decrease in IC
50
value as against free PTX when incubated for 72 h. The apoptotic index in case of PTX-TPGS-LNC was ~ twofold higher than free PTX. The pharmacokinetic profile of PTX-TPGS-LNC revealed a ~ 3.18-fold increase in
t
1/2
and a ~ 2.62-fold higher AUC
(0→∞)
compared to Intaxel
®
. Finally, treatment with PTX-TPGS-LNC demonstrated significant lowering in the % tumor burden and serum toxicity markers compared to marketed formulation Intaxel
®
. Thus, the lipid- and TPGS-based core–shell-type LNC with high PTX loading can advance the existing standards of therapy for overshadowing cancer.
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d
-α-tocopheryl polyethylene glycol succinate (TPGS)–based core–shell-type lipid nanocapsules (PTX-TPGS-LNC) for augmenting the therapeutic efficacy and curbing the toxicity. PTX-TPGS-LNCs were formulated by employing anti-solvent precipitation technique and displayed a particle size of 162.1 ± 4.70 nm and % practical drug loading of 15.04 ± 2.44%. Electron microscopy revealed that PTX-TPGS-LNCs have spherical morphology and the inner core was surrounded by a relatively lighter region, i.e., layer of lipids and TPGS. The nature of loaded PTX inside the PTX-TPGS-LNC was also confirmed using DSC and PXRD analysis. The
in vitro
release study showed biphasic and sustained release pattern of PTX from PTX-TPGS-LNC and it showed ~ threefold higher PTX uptake in MCF-7 cell line in comparison to free PTX. Moreover, it was apparent from the cytotoxicity assay that PTX-TPGS-LNC displayed higher cytotoxicity in MCF-7 cells and revealed ~ 2.92-fold decrease in IC
50
value as against free PTX when incubated for 72 h. The apoptotic index in case of PTX-TPGS-LNC was ~ twofold higher than free PTX. The pharmacokinetic profile of PTX-TPGS-LNC revealed a ~ 3.18-fold increase in
t
1/2
and a ~ 2.62-fold higher AUC
(0→∞)
compared to Intaxel
®
. Finally, treatment with PTX-TPGS-LNC demonstrated significant lowering in the % tumor burden and serum toxicity markers compared to marketed formulation Intaxel
®
. Thus, the lipid- and TPGS-based core–shell-type LNC with high PTX loading can advance the existing standards of therapy for overshadowing cancer.
Graphical abstract</description><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Research Article</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><recordid>eNp9kM1OAjEUhSdGExF9AVdduqn2Z5ifJRIUE6Ik4LrptBcoGdqxHYLEje_gG_okFnDhysXNvTf5zknOSZJrSm4pI8VdoIylJSaMxeFFidOTpEN7nOCy5Oz0z32eXISwIpGiJe8kH2PTGI2RtBrNJo9TfC8DaDRwHr4_v6ZLqGs82zWAnqV1SjZhU0NAQ6vdNmJb0y7RyCyWaCJVbVr5DjUaO6mNXRwsh3YprYpk37ZG7U-PJq6F-Mn6MjmbyzrA1e_uJq8Pw9lghMcvj0-D_hgrztIW51BUaVr1gPfmWimmS17kutCqzHXaKyArGGF5VlWSkwpUWWSQUUkyzVSWVhR4N7k5-jbevW0gtGJtgorJpAW3CYLlJMtpximLKDuiyrsQPMxF481a-p2gROybFsemRWxaHJoWaRTxoyhE2C7Ai5XbeBsj_af6AVr1gsI</recordid><startdate>20220824</startdate><enddate>20220824</enddate><creator>Katiyar, Sameer S.</creator><creator>Patil, Ravindra</creator><creator>Ghadi, Rohan</creator><creator>Kuche, Kaushik</creator><creator>Kushwah, Varun</creator><creator>Dora, Chander Parkash</creator><creator>Jain, Sanyog</creator><general>Springer International Publishing</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-0688-9563</orcidid></search><sort><creationdate>20220824</creationdate><title>Lipid- and TPGS-Based Core–Shell-Type Nanocapsules Endowed with High Paclitaxel Loading and Enhanced Anticancer Potential</title><author>Katiyar, Sameer S. ; Patil, Ravindra ; Ghadi, Rohan ; Kuche, Kaushik ; Kushwah, Varun ; Dora, Chander Parkash ; Jain, Sanyog</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c324t-7e8b44b5e35fdcc2d9387d8dc97d458e6820276bba30bec986e61a06d2c64b1e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Research Article</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Katiyar, Sameer S.</creatorcontrib><creatorcontrib>Patil, Ravindra</creatorcontrib><creatorcontrib>Ghadi, Rohan</creatorcontrib><creatorcontrib>Kuche, Kaushik</creatorcontrib><creatorcontrib>Kushwah, Varun</creatorcontrib><creatorcontrib>Dora, Chander Parkash</creatorcontrib><creatorcontrib>Jain, Sanyog</creatorcontrib><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Katiyar, Sameer S.</au><au>Patil, Ravindra</au><au>Ghadi, Rohan</au><au>Kuche, Kaushik</au><au>Kushwah, Varun</au><au>Dora, Chander Parkash</au><au>Jain, Sanyog</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Lipid- and TPGS-Based Core–Shell-Type Nanocapsules Endowed with High Paclitaxel Loading and Enhanced Anticancer Potential</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><date>2022-08-24</date><risdate>2022</risdate><volume>23</volume><issue>7</issue><spage>238</spage><epage>238</epage><pages>238-238</pages><artnum>238</artnum><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>The current study elucidates the improved drug loading of paclitaxel (PTX) in lipid- and
d
-α-tocopheryl polyethylene glycol succinate (TPGS)–based core–shell-type lipid nanocapsules (PTX-TPGS-LNC) for augmenting the therapeutic efficacy and curbing the toxicity. PTX-TPGS-LNCs were formulated by employing anti-solvent precipitation technique and displayed a particle size of 162.1 ± 4.70 nm and % practical drug loading of 15.04 ± 2.44%. Electron microscopy revealed that PTX-TPGS-LNCs have spherical morphology and the inner core was surrounded by a relatively lighter region, i.e., layer of lipids and TPGS. The nature of loaded PTX inside the PTX-TPGS-LNC was also confirmed using DSC and PXRD analysis. The
in vitro
release study showed biphasic and sustained release pattern of PTX from PTX-TPGS-LNC and it showed ~ threefold higher PTX uptake in MCF-7 cell line in comparison to free PTX. Moreover, it was apparent from the cytotoxicity assay that PTX-TPGS-LNC displayed higher cytotoxicity in MCF-7 cells and revealed ~ 2.92-fold decrease in IC
50
value as against free PTX when incubated for 72 h. The apoptotic index in case of PTX-TPGS-LNC was ~ twofold higher than free PTX. The pharmacokinetic profile of PTX-TPGS-LNC revealed a ~ 3.18-fold increase in
t
1/2
and a ~ 2.62-fold higher AUC
(0→∞)
compared to Intaxel
®
. Finally, treatment with PTX-TPGS-LNC demonstrated significant lowering in the % tumor burden and serum toxicity markers compared to marketed formulation Intaxel
®
. Thus, the lipid- and TPGS-based core–shell-type LNC with high PTX loading can advance the existing standards of therapy for overshadowing cancer.
Graphical abstract</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><doi>10.1208/s12249-022-02389-4</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0002-0688-9563</orcidid></addata></record> |
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| subjects | Biochemistry Biomedical and Life Sciences Biomedicine Biotechnology Pharmacology/Toxicology Pharmacy Research Article |
| title | Lipid- and TPGS-Based Core–Shell-Type Nanocapsules Endowed with High Paclitaxel Loading and Enhanced Anticancer Potential |
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