EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma

Shumin Li; Zhongkai Xu; Majed Alrobaian; Obaid Afzal; Imran Kazmi; Waleed H. Almalki; Abdulmalik Saleh Alfawaz Altamimi; Fahad A. Al-Abbasi; Khalid S. Alharbi; Waleed M. Altowayan; Tanuja Singh; Md Habban Akhter; Manish Gupta; Mahfoozur Rahman; Sarwar Beg

doi:10.1002/bab.2279

EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma

Shumin Li, Zhongkai Xu, Majed Alrobaian, Obaid Afzal, Imran Kazmi, Waleed H. Almalki, Abdulmalik Saleh Alfawaz Altamimi, Fahad A. Al-Abbasi, Khalid S. Alharbi, Waleed M. Altowayan, Tanuja Singh, Md Habban Akhter, Manish Gupta, Mahfoozur Rahman, Sarwar Beg

Pharmaceutical Chemistry

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19 Scopus citations

Abstract

The present research work describes development of dual drug-loaded lipid–polymer hybrid nanoparticles (LPHNPs) of anticancer therapeutics for the management of colon cancer. The epidermal growth factor (EGF)-functionalized LPHNPs coloaded with 5-fluorouracil (FU) and sulforaphane (SFN) were prepared by one-step nanoprecipitation method. Box–Behnken design was applied for optimizing the material attributes and process parameters. The optimized LPHNPs revealed particle size 198 nm, polydispersity index 0.3, zeta potential. −25.3 mV, and drug loading efficiency 19–20.3% for 5-FU and SFN, respectively. EGF functionalization on LPHNPs was confirmed from positive magnitude of zeta potential to 21.3 mV as compared with the plain LPHNPs. In vitro drug release performance indicated sustained and non-Fickian mechanism release nature of the drugs from LPHNPs. Anticancer activity evaluation in HCT-15 colon cancer cells showed significant reduction (p < 0.001) in the cell growth and cytotoxicity of the investigated drugs from various treatments in the order: EGF-functionalized LPHNPs > plain LPHNPs > free drug suspensions. Overall, the research work corroborated improved treatment efficacy of EGF-functionalized LPHNPs for delivering chemotherapeutic agents for the management of colon carcinoma.

Original language	English
Pages (from-to)	2205-2221
Number of pages	17
Journal	Biotechnology and Applied Biochemistry
Volume	69
Issue number	5
DOIs	https://doi.org/10.1002/bab.2279
State	Published - Oct 2022

Keywords

active targeting
colon cancer
drug delivery
hybrid nanoparticles
quality by design

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/bab.2279

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Li, S., Xu, Z., Alrobaian, M., Afzal, O., Kazmi, I., Almalki, W. H., Altamimi, A. S. A., Al-Abbasi, F. A., Alharbi, K. S., Altowayan, W. M., Singh, T., Akhter, M. H., Gupta, M., Rahman, M., & Beg, S. (2022). EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma. Biotechnology and Applied Biochemistry, 69(5), 2205-2221. https://doi.org/10.1002/bab.2279

@article{96921c9f373d420d87747e36297f72c4,

title = "EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma",

abstract = "The present research work describes development of dual drug-loaded lipid–polymer hybrid nanoparticles (LPHNPs) of anticancer therapeutics for the management of colon cancer. The epidermal growth factor (EGF)-functionalized LPHNPs coloaded with 5-fluorouracil (FU) and sulforaphane (SFN) were prepared by one-step nanoprecipitation method. Box–Behnken design was applied for optimizing the material attributes and process parameters. The optimized LPHNPs revealed particle size 198 nm, polydispersity index 0.3, zeta potential. −25.3 mV, and drug loading efficiency 19–20.3\% for 5-FU and SFN, respectively. EGF functionalization on LPHNPs was confirmed from positive magnitude of zeta potential to 21.3 mV as compared with the plain LPHNPs. In vitro drug release performance indicated sustained and non-Fickian mechanism release nature of the drugs from LPHNPs. Anticancer activity evaluation in HCT-15 colon cancer cells showed significant reduction (p < 0.001) in the cell growth and cytotoxicity of the investigated drugs from various treatments in the order: EGF-functionalized LPHNPs > plain LPHNPs > free drug suspensions. Overall, the research work corroborated improved treatment efficacy of EGF-functionalized LPHNPs for delivering chemotherapeutic agents for the management of colon carcinoma.",

keywords = "active targeting, colon cancer, drug delivery, hybrid nanoparticles, quality by design",

author = "Shumin Li and Zhongkai Xu and Majed Alrobaian and Obaid Afzal and Imran Kazmi and Almalki, \{Waleed H.\} and Altamimi, \{Abdulmalik Saleh Alfawaz\} and Al-Abbasi, \{Fahad A.\} and Alharbi, \{Khalid S.\} and Altowayan, \{Waleed M.\} and Tanuja Singh and Akhter, \{Md Habban\} and Manish Gupta and Mahfoozur Rahman and Sarwar Beg",

note = "Publisher Copyright: {\textcopyright} 2021 International Union of Biochemistry and Molecular Biology, Inc.",

year = "2022",

month = oct,

doi = "10.1002/bab.2279",

language = "English",

volume = "69",

pages = "2205--2221",

journal = "Biotechnology and Applied Biochemistry",

issn = "0885-4513",

publisher = "Wiley-Blackwell",

number = "5",

}

Li, S, Xu, Z, Alrobaian, M, Afzal, O, Kazmi, I, Almalki, WH, Altamimi, ASA, Al-Abbasi, FA, Alharbi, KS, Altowayan, WM, Singh, T, Akhter, MH, Gupta, M, Rahman, M & Beg, S 2022, 'EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma', Biotechnology and Applied Biochemistry, vol. 69, no. 5, pp. 2205-2221. https://doi.org/10.1002/bab.2279

EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma. / Li, Shumin; Xu, Zhongkai; Alrobaian, Majed et al.
In: Biotechnology and Applied Biochemistry, Vol. 69, No. 5, 10.2022, p. 2205-2221.

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

TY - JOUR

T1 - EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma

AU - Li, Shumin

AU - Xu, Zhongkai

AU - Alrobaian, Majed

AU - Afzal, Obaid

AU - Kazmi, Imran

AU - Almalki, Waleed H.

AU - Altamimi, Abdulmalik Saleh Alfawaz

AU - Al-Abbasi, Fahad A.

AU - Alharbi, Khalid S.

AU - Altowayan, Waleed M.

AU - Singh, Tanuja

AU - Akhter, Md Habban

AU - Gupta, Manish

AU - Rahman, Mahfoozur

AU - Beg, Sarwar

PY - 2022/10

Y1 - 2022/10

N2 - The present research work describes development of dual drug-loaded lipid–polymer hybrid nanoparticles (LPHNPs) of anticancer therapeutics for the management of colon cancer. The epidermal growth factor (EGF)-functionalized LPHNPs coloaded with 5-fluorouracil (FU) and sulforaphane (SFN) were prepared by one-step nanoprecipitation method. Box–Behnken design was applied for optimizing the material attributes and process parameters. The optimized LPHNPs revealed particle size 198 nm, polydispersity index 0.3, zeta potential. −25.3 mV, and drug loading efficiency 19–20.3% for 5-FU and SFN, respectively. EGF functionalization on LPHNPs was confirmed from positive magnitude of zeta potential to 21.3 mV as compared with the plain LPHNPs. In vitro drug release performance indicated sustained and non-Fickian mechanism release nature of the drugs from LPHNPs. Anticancer activity evaluation in HCT-15 colon cancer cells showed significant reduction (p < 0.001) in the cell growth and cytotoxicity of the investigated drugs from various treatments in the order: EGF-functionalized LPHNPs > plain LPHNPs > free drug suspensions. Overall, the research work corroborated improved treatment efficacy of EGF-functionalized LPHNPs for delivering chemotherapeutic agents for the management of colon carcinoma.

AB - The present research work describes development of dual drug-loaded lipid–polymer hybrid nanoparticles (LPHNPs) of anticancer therapeutics for the management of colon cancer. The epidermal growth factor (EGF)-functionalized LPHNPs coloaded with 5-fluorouracil (FU) and sulforaphane (SFN) were prepared by one-step nanoprecipitation method. Box–Behnken design was applied for optimizing the material attributes and process parameters. The optimized LPHNPs revealed particle size 198 nm, polydispersity index 0.3, zeta potential. −25.3 mV, and drug loading efficiency 19–20.3% for 5-FU and SFN, respectively. EGF functionalization on LPHNPs was confirmed from positive magnitude of zeta potential to 21.3 mV as compared with the plain LPHNPs. In vitro drug release performance indicated sustained and non-Fickian mechanism release nature of the drugs from LPHNPs. Anticancer activity evaluation in HCT-15 colon cancer cells showed significant reduction (p < 0.001) in the cell growth and cytotoxicity of the investigated drugs from various treatments in the order: EGF-functionalized LPHNPs > plain LPHNPs > free drug suspensions. Overall, the research work corroborated improved treatment efficacy of EGF-functionalized LPHNPs for delivering chemotherapeutic agents for the management of colon carcinoma.

KW - active targeting

KW - colon cancer

KW - drug delivery

KW - hybrid nanoparticles

KW - quality by design

UR - http://www.scopus.com/inward/record.url?scp=85119842552&partnerID=8YFLogxK

U2 - 10.1002/bab.2279

DO - 10.1002/bab.2279

M3 - Article

C2 - 34775646

AN - SCOPUS:85119842552

SN - 0885-4513

VL - 69

SP - 2205

EP - 2221

JO - Biotechnology and Applied Biochemistry

JF - Biotechnology and Applied Biochemistry

IS - 5

ER -

EGF-functionalized lipid–polymer hybrid nanoparticles of 5-fluorouracil and sulforaphane with enhanced bioavailability and anticancer activity against colon carcinoma

Abstract

Keywords

UN SDGs

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