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Article

Enhancement of Anti-Tumoral Properties of Paclitaxel Nano-Crystals by Conjugation of Folic Acid to Pluronic F127: Formulation Optimization, In Vitro and In Vivo Study

by
Nagaraja Sreeharsha
1,2,*,†,
Samathoti Prasanthi
3,
Satyavarapu Veera Venkata Naga Satya Mahalakshmi
4,
Prakash S. Goudanavar
5,†,
Nimbagal Raghavendra Naveen
5,*,
Buduru Gowthami
6,
Santosh Fattepur
7,*,
Girish Meravanige
8,
Syed Mohammed Basheeruddin Asdaq
9,
Md. Khalid Anwer
10,
Bandar Aldhubiab
1,
Mohammed Monirul Islam
11,
Mohammed Habeebuddin
8,
Mallikarjun Telsang
12,
Mazen Al Gharsan
1 and
Michelyne Haroun
1
1
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Hofuf 31982, Saudi Arabia
2
Department of Pharmaceutics, Vidya Siri College of Pharmacy, Off Sarjapura Road, Bangalore 560035, Karnataka, India
3
Department of Pharmaceutics, Sri Venkateswara College of Pharmacy, RVS Nagar, Tirupati Rd, Chittoor 517127, Andhra Pradesh, India
4
Department of pharmacognosy, Vishnu Institute of Pharmaceutical Education and Research, Narsapur, Medak 502313, Telangana, India
5
Department of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, Mandava 571448, Karnataka, India
6
Department of Pharmaceutics, Annamacharya College of Pharmacy, New Boyanapalli, Rajampet 516126, Andhra Pradesh, India
7
School of Pharmacy, Management and Science University, Seksyen 13, Shah Alam 40100, Selangor, Malaysia
8
Department of Biomedical Sciences, College of Medicine, King Faisal University, Al Hofuf 31982, Saudi Arabia
9
Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Dariyah, Riyadh 13713, Saudi Arabia
10
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Alkharj 11942, Saudi Arabia
11
Department of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al Hofuf 31982, Saudi Arabia
12
Department of Surgery, College of Medicine, King Faisal University, Al Hofuf 31982, Saudi Arabia
 
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*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2022, 27(22), 7914; https://doi.org/10.3390/molecules27227914
Submission received: 1 October 2022 / Revised: 28 October 2022 / Accepted: 2 November 2022 / Published: 16 November 2022
(This article belongs to the Section Applied Chemistry)
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Abstract

A brand-new nano-crystal (NC) version of the hydrophobic drug Paclitaxel (PT) were formulated for cancer treatment. A stable NC formulation for the administration of PT was created using the triblock co-polymer Pluronic F127. To achieve maximum entrapment effectiveness and minimal particle size, the formulation was improved using the central composite design by considering agitation speed and vacuum pressure at five levels (coded as +1.414, +1, 0, −1, and −1.414). According to the Design Expert software’s predictions, 13 runs were created and evaluated for the chosen responses. The formulation prepared with an agitation speed of 1260 RPM and a vacuum pressure of 77.53 mbar can meet the requirements of the ideal formulation in order to achieve 142.56 nm of PS and 75.18% EE, according to the level of desirability (D = 0.959). Folic acid was conjugated to Pluronic F127 to create folate receptor-targeted NC. The drug release profile of the nano-crystals in vitro demonstrated sustained release over an extended period. Folate receptor (FR)-targeted NC (O-PT-NC-Folate) has also been prepared by conjugating folic acid to Pluronic F127. MTT test is used to validate the targeting efficacy on the FR-positive human oral cancer cell line (KB). At pharmacologically relevant concentrations, the PT nano-crystal formulation did not cause hemolysis. Compared to non-targeted NC of PT, the O-PT-NC-Folate showed a comparable but more sustained anti-cancer effect, according to an in vivo anti-tumor investigation in NCI/ADR-RES cell lines. The remarkable anti-tumor effectiveness, minimal toxicity, and simplicity of scale-up manufacturing of the NC formulations indicate their potential for clinical development. Other hydrophobic medications that are formulated into nano-systems for improved therapy may benefit from the formulation approach.
Keywords: nano-crystals; Paclitaxel; anti-cancer; optimization; central composite design nano-crystals; Paclitaxel; anti-cancer; optimization; central composite design

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MDPI and ACS Style

Sreeharsha, N.; Prasanthi, S.; Mahalakshmi, S.V.V.N.S.; Goudanavar, P.S.; Naveen, N.R.; Gowthami, B.; Fattepur, S.; Meravanige, G.; Asdaq, S.M.B.; Anwer, M.K.; et al. Enhancement of Anti-Tumoral Properties of Paclitaxel Nano-Crystals by Conjugation of Folic Acid to Pluronic F127: Formulation Optimization, In Vitro and In Vivo Study. Molecules 2022, 27, 7914. https://doi.org/10.3390/molecules27227914

AMA Style

Sreeharsha N, Prasanthi S, Mahalakshmi SVVNS, Goudanavar PS, Naveen NR, Gowthami B, Fattepur S, Meravanige G, Asdaq SMB, Anwer MK, et al. Enhancement of Anti-Tumoral Properties of Paclitaxel Nano-Crystals by Conjugation of Folic Acid to Pluronic F127: Formulation Optimization, In Vitro and In Vivo Study. Molecules. 2022; 27(22):7914. https://doi.org/10.3390/molecules27227914

Chicago/Turabian Style

Sreeharsha, Nagaraja, Samathoti Prasanthi, Satyavarapu Veera Venkata Naga Satya Mahalakshmi, Prakash S. Goudanavar, Nimbagal Raghavendra Naveen, Buduru Gowthami, Santosh Fattepur, Girish Meravanige, Syed Mohammed Basheeruddin Asdaq, Md. Khalid Anwer, and et al. 2022. "Enhancement of Anti-Tumoral Properties of Paclitaxel Nano-Crystals by Conjugation of Folic Acid to Pluronic F127: Formulation Optimization, In Vitro and In Vivo Study" Molecules 27, no. 22: 7914. https://doi.org/10.3390/molecules27227914

APA Style

Sreeharsha, N., Prasanthi, S., Mahalakshmi, S. V. V. N. S., Goudanavar, P. S., Naveen, N. R., Gowthami, B., Fattepur, S., Meravanige, G., Asdaq, S. M. B., Anwer, M. K., Aldhubiab, B., Islam, M. M., Habeebuddin, M., Telsang, M., Gharsan, M. A., & Haroun, M. (2022). Enhancement of Anti-Tumoral Properties of Paclitaxel Nano-Crystals by Conjugation of Folic Acid to Pluronic F127: Formulation Optimization, In Vitro and In Vivo Study. Molecules, 27(22), 7914. https://doi.org/10.3390/molecules27227914

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