Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery

Hari Krishnareddy Rachamalla; Santanu Bhattacharya; Ajaz Ahmad; Kathyayani Sridharan; Vijay Sagar Madamsetty; Sujan Kumar Mondal; Enfeng Wang; Shamit K. Dutta; Basit L. Jan; Sudhakar Jinka; Madan Mohan Chandra Sekhar Jaggarapu; Venu Yakati; Debabrata Mukhopadhyay; Khalid M. Alkharfy; Rajkumar Banerjee

doi:10.2217/nnm-2020-0470

Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery

Hari Krishnareddy Rachamalla, Santanu Bhattacharya, Ajaz Ahmad, Kathyayani Sridharan, Vijay Sagar Madamsetty, Sujan Kumar Mondal, Enfeng Wang, Shamit K. Dutta, Basit L. Jan, Sudhakar Jinka, Madan Mohan Chandra Sekhar Jaggarapu, Venu Yakati, Debabrata Mukhopadhyay, Khalid M. Alkharfy, Rajkumar Banerjee

Research output: Contribution to journal › Article › peer-review

Abstract

Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.

Original language	English (US)
Pages (from-to)	641-656
Number of pages	16
Journal	Nanomedicine
Volume	16
Issue number	8
DOIs	https://doi.org/10.2217/nnm-2020-0470
State	Published - Apr 2021

Keywords

cationic lipid
liposomes
pancreatic cancer
pharmacokinetic evaluation
thymoquinone

ASJC Scopus subject areas

Bioengineering
Development
Biomedical Engineering
General Materials Science
Medicine (miscellaneous)

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Rachamalla, H. K., Bhattacharya, S., Ahmad, A., Sridharan, K., Madamsetty, V. S., Mondal, S. K., Wang, E., Dutta, S. K., Jan, B. L., Jinka, S., Chandra Sekhar Jaggarapu, M. M., Yakati, V., Mukhopadhyay, D., Alkharfy, K. M., & Banerjee, R. (2021). Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery. Nanomedicine, 16(8), 641-656. https://doi.org/10.2217/nnm-2020-0470

Rachamalla, HK, Bhattacharya, S, Ahmad, A, Sridharan, K, Madamsetty, VS, Mondal, SK, Wang, E, Dutta, SK, Jan, BL, Jinka, S, Chandra Sekhar Jaggarapu, MM, Yakati, V, Mukhopadhyay, D, Alkharfy, KM & Banerjee, R 2021, 'Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery', Nanomedicine, vol. 16, no. 8, pp. 641-656. https://doi.org/10.2217/nnm-2020-0470

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title = "Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery",

abstract = "Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.",

keywords = "cationic lipid, liposomes, pancreatic cancer, pharmacokinetic evaluation, thymoquinone",

author = "Rachamalla, {Hari Krishnareddy} and Santanu Bhattacharya and Ajaz Ahmad and Kathyayani Sridharan and Madamsetty, {Vijay Sagar} and Mondal, {Sujan Kumar} and Enfeng Wang and Dutta, {Shamit K.} and Jan, {Basit L.} and Sudhakar Jinka and {Chandra Sekhar Jaggarapu}, {Madan Mohan} and Venu Yakati and Debabrata Mukhopadhyay and Alkharfy, {Khalid M.} and Rajkumar Banerjee",

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year = "2021",

month = apr,

doi = "10.2217/nnm-2020-0470",

language = "English (US)",

volume = "16",

pages = "641--656",

journal = "Nanomedicine",

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TY - JOUR

T1 - Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery

AU - Rachamalla, Hari Krishnareddy

AU - Bhattacharya, Santanu

AU - Ahmad, Ajaz

AU - Sridharan, Kathyayani

AU - Madamsetty, Vijay Sagar

AU - Mondal, Sujan Kumar

AU - Wang, Enfeng

AU - Dutta, Shamit K.

AU - Jan, Basit L.

AU - Jinka, Sudhakar

AU - Chandra Sekhar Jaggarapu, Madan Mohan

AU - Yakati, Venu

AU - Mukhopadhyay, Debabrata

AU - Alkharfy, Khalid M.

AU - Banerjee, Rajkumar

PY - 2021/4

Y1 - 2021/4

N2 - Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.

AB - Background: Thymoquinone (TQ) has potential anti-inflammatory, immunomodulatory and anticancer effects but its clinical use is limited by its low solubility, poor bioavailability and rapid clearance. Aim: To enhance systemic bioavailability and tumor-specific toxicity of TQ. Materials & methods: Cationic liposomal formulation of TQ (D1T) was prepared via ethanol injection method and their physicochemical properties, anticancer effects in orthotopic xenograft pancreatic tumor model and pharmacokinetic behavior of D1T relative to TQ were evaluated. Results: D1T showed prominent inhibition of pancreatic tumor progression, significantly greater in vivo absorption, approximately 1.5-fold higher plasma concentration, higher bioavailability, reduced volume of distribution and improved clearance relative to TQ. Conclusion: Encapsulation of TQ in cationic liposomal formulation enhanced its bioavailability and anticancer efficacy against xenograft pancreatic tumor.

KW - cationic lipid

KW - liposomes

KW - pancreatic cancer

KW - pharmacokinetic evaluation

KW - thymoquinone

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JO - Nanomedicine

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Enriched pharmacokinetic behavior and antitumor efficacy of thymoquinone by liposomal delivery

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