Synthesis of Methotrexate Loaded Chitosan Nanoparticles and in vitro Evaluation of the Potential in Treatment of Prostate Cancer

Nur, Selvi Gunel; Özel, Buket; Kıpçak, Sezgi; Aktan, Çağdaş; Cansu, Akgun; Guliz, Ak; Yılmaz, Habibe; Cigir, Biray Avci; Dodurga, Yavuz; Şanlıer, Şenay Hamarat

doi:10.2174/1871520616666160101120040

“…In prior studies, the ionic gelation process was used to create methotrexate-encapsulated Cs nanoparticles tested in vitro against the LNCaP cell line. 26 A related method was used to assess the cytotoxic effects of VC-encapsulated folic acid-Cs linked nanomaterials on NCI-H460 cells. 27 …”

Section: Resultsmentioning

confidence: 99%

Anticancer Analysis of CD44 Targeted Cyclosporine Loaded Thiolated Chitosan Nanoformulations for Sustained Release in Triple-Negative Breast Cancer

Abduh

2023

IJN

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Introduction Cyclosporine (CsA), a potent immunosuppressive chemotherapeutic medication, treats numerous cancers, particularly malignant carcinoma, acute leukemia, and triple-negative breast cancer (TNBC). Methodology A specified polymeric nanoformulation (NF) based drug delivery technique with ligand functionalization at the surface was developed to improve its delivery at the intended area and boost the efficacy for prolonged time. The in silico verified the HA binding to the CD44 receptor at binding sites A and B in triple-negative breast cancer cells. The NF of encapsulated Cyclosporine in thiolated chitosan (TC) with the outermost coating of hyaluronic acid (HA) was formulated and characterized. Results So, the zeta analysis revealed a particle size of 192 nm and PDI of 0.433, zeta potential of 38.9mV. FTIR and Raman investigations also support the existence of hydrophobic groups, porous surfaces, and non-clumping characteristics. While XRD verified its crystallographic nature while SEM and TEM analysis revealed the spherical nanoparticles with sleek exteriors. DSC demonstrated the stability of NF at high temperatures. The NF showed 85% drug encapsulation followed Higuchi release model for therapeutic moiety at acidic pH for a maximum of 72 hours. When compared to raw Cyclosporine, the in vitro tumor cell inhibition of ThC-HA encapsulated with Cyclosporine was tested using an MTT dye on normal breast epithelial cells compared to triple-negative breast cancer cells. Conclusion This novel formulation improved the long-term viability, effectiveness, and active targeting as an effective and potent therapeutic moiety against cancer.

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“…The nanoformulations of Cyclosporin were formulated through an ionic gelation process without using harsh chemicals and with no energy expenditure following green synthesis protocols. In prior studies, the ionic gelation process was used to create methotrexate-encapsulated Cs nanoparticles tested in-vitro against the LNCaP cell line [26]. A related method assessed the cytotoxic effects of Vincristine encapsulated folic acid-Cs-linked nanomaterials on NCI-H460 cells [27].…”

Section: Discussionmentioning

confidence: 99%

Anticancer analysis of CD44 targeted Cyclosporine loaded thiolated chitosan nanoformulations for sustained release in triple-negative breast cancer.

Abduh

2023

Preprint

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Cyclosporine (CsA), a potent immunosuppressive chemotherapeutic medication, treats numerous cancers, particularly malignant carcinoma, acute leukemia, and triple-negative breast cancer (TNBC). A specified polymeric nanoformulation (N.F.) based drug delivery technique with ligand alteration at the surface was developed to improve active moiety delivery at the intended area and boost the efficacy of prolonged treatment. We produced and characterized N.F. of encapsulated Cyclosporine in thiolated chitosan (T.C.) with the outermost coating of hyaluronic acid (H.A.). Research in-silico verified that H.A. binds to the receptor CD44 at docking locations A and B in triple-negative breast cancer cells. When a pharmaceutical substance interacts with a polymeric compound, zeta examination reveals a particle size of 192nm, a PDI of 0.433, and zeta potential of 38.9 mV. FTIR and Raman's investigations also support the existence of hydrophobic groups, porous surfaces, and clumping characteristics. While XRD verified its crystallographic nature, which renders N.F. particularly helpful in localized drug delivery systems (DDS), SEM and TEM revealed circular nanoparticles with sleek exteriors. DSC demonstrated that N.F. was stable at high temperature. The NF showed 85% drug encapsulation, and a kinetics investigation of drug release revealed that the N.F. obeyed the Higuchi model for dispersion at low pH. In contrast to typical CsA's immediate release in under 12 hours, the in-vitro investigation demonstrated prolonged continuous dissolution at pH 7.4 and 6.8 for a maximum of 72 hours. When compared to raw Cyclosporine, the in-vitro tumor prevention properties of the ThC-HA encapsulated with Cyclosporine were tested using an MTT test on normal breast epithelial cells and triple-negative breast cancer cells. It showed the synthesized N.F.'s robust cytotoxic potential at reduced concentrations and its effectiveness for normal cells. These characteristics improve the long-term viability, effectiveness, and active targeting of prepared novel N.F.s as an effective pharmaceutical component and potent therapeutic moiety against cancer.

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“…In prior studies, the ionic gelation process was used to create methotrexate-encapsulated Cs nanoparticles tested in vitro against the LNCaP cell line. 26 A related method was used to assess the cytotoxic effects of VC-encapsulated folic acid-Cs linked nanomaterials on NCI-H460 cells. 27…”

Section: Synthesis Of Nanoformulations Of Blank and Csa Encapsulated ...mentioning

confidence: 99%

Anticancer analysis of CD44 targeted Cyclosporine loaded thiolated chitosan nanoformulations for sustained release in triple-negative breast cancer.

Abduh

¹

2023

Preprint

1

0

View full text Add to dashboard Cite

Cyclosporine (CsA), a potent immunosuppressive chemotherapeutic medication, treats numerous cancers, particularly malignant carcinoma, acute leukemia, and triple-negative breast cancer (TNBC). A specified polymeric nanoformulation (N.F.) based drug delivery technique with ligand alteration at the surface was developed to improve active moiety delivery at the intended area and boost the efficacy of prolonged treatment. We produced and characterized N.F. of encapsulated Cyclosporine in thiolated chitosan (T.C.) with the outermost coating of hyaluronic acid (H.A.). Research in-silico verified that H.A. binds to the receptor CD44 at docking locations A and B in triple-negative breast cancer cells. When a pharmaceutical substance interacts with a polymeric compound, zeta examination reveals a particle size of 192nm, a PDI of 0.433, and zeta potential of 38.9 mV. FTIR and Raman's investigations also support the existence of hydrophobic groups, porous surfaces, and clumping characteristics. While XRD verified its crystallographic nature, which renders N.F. particularly helpful in localized drug delivery systems (DDS), SEM and TEM revealed circular nanoparticles with sleek exteriors. DSC demonstrated that N.F. was stable at high temperature. The NF showed 85% drug encapsulation, and a kinetics investigation of drug release revealed that the N.F. obeyed the Higuchi model for dispersion at low pH. In contrast to typical CsA's immediate release in under 12 hours, the in-vitro investigation demonstrated prolonged continuous dissolution at pH 7.4 and 6.8 for a maximum of 72 hours. When compared to raw Cyclosporine, the in-vitro tumor prevention properties of the ThC-HA encapsulated with Cyclosporine were tested using an MTT test on normal breast epithelial cells and triple-negative breast cancer cells. It showed the synthesized N.F.'s robust cytotoxic potential at reduced concentrations and its effectiveness for normal cells. These characteristics improve the long-term viability, effectiveness, and active targeting of prepared novel N.F.s as an effective pharmaceutical component and potent therapeutic moiety against cancer.

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Synthesis of Methotrexate Loaded Chitosan Nanoparticles and in vitro Evaluation of the Potential in Treatment of Prostate Cancer

Cited by 14 publications

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Anticancer Analysis of CD44 Targeted Cyclosporine Loaded Thiolated Chitosan Nanoformulations for Sustained Release in Triple-Negative Breast Cancer

Anticancer Analysis of CD44 Targeted Cyclosporine Loaded Thiolated Chitosan Nanoformulations for Sustained Release in Triple-Negative Breast Cancer

Anticancer analysis of CD44 targeted Cyclosporine loaded thiolated chitosan nanoformulations for sustained release in triple-negative breast cancer.

Anticancer analysis of CD44 targeted Cyclosporine loaded thiolated chitosan nanoformulations for sustained release in triple-negative breast cancer.

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