Exploring fatty acid-amino acid conjugate for the development of self-assembling, pH-sensitive vesicles for targeted anticancer drug delivery
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Neela M. Bhatia
Dr. Neela M. Bhatia: Working as Professor in Department of Quality Assurance at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Ms. Ashwini Shekhar: Master research scholar in Department of Quality Assurance at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Ms. Pallavi Mane: Master research scholar in Department of Quality Assurance at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Dr. Manish S. Bhatia: Working as Professor in Department of Pharmaceutical Chemistry at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Dr. Vinod L. Gaikwad: Working as Assistant Professor in Department of Pharmaceutics at National Institute of Pharmaceutical Education and Research (NIPER) Hajipur, Bihar, India.
Abstract
A novel, pH-sensitive ‘fatty acid-amino acid conjugate’ (L-arginine oleoyl acid amide) was synthesized. The conjugate was evaluated for its suitability as a carrier in the development of a biocompatible and pH-responsive vesicular system for tumor-targeted delivery of pazopanib hydrochloride (PHC). Prepared vesicles exhibited high drug encapsulation efficiency (83.3 %) and a pH-dependent phase transition at the acidic pH of the tumor microenvironment. Formulated vesicles showed a high rate of PHC release in the acidic media (pH 5 > 6.8 > 7.4) similar to the pH of the tumor site, indicating more accurate and selective drug delivery. The vesicles showed a PHC concentration-dependent effect on the viability of ACHN/A498 human renal cancer cells and significantly high intracellular uptake of PHC (83.07 %). Therefore, the developed pH-activated vesicular drug delivery system with predetermined fatty acid-amino acid composition in conjugate could serve as a promising controlled and targeted delivery approach for PHC and other anticancer drugs.
About the authors
Dr. Neela M. Bhatia: Working as Professor in Department of Quality Assurance at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Ms. Ashwini Shekhar: Master research scholar in Department of Quality Assurance at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Ms. Pallavi Mane: Master research scholar in Department of Quality Assurance at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Dr. Manish S. Bhatia: Working as Professor in Department of Pharmaceutical Chemistry at Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India.
Dr. Vinod L. Gaikwad: Working as Assistant Professor in Department of Pharmaceutics at National Institute of Pharmaceutical Education and Research (NIPER) Hajipur, Bihar, India.
Acknowledgments
The authors are grateful to Hetero Labs Limited, Visakhapatnam, India, for providing a gift sample of Pazopanib hydrochloride.
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Research ethics: Not applicable.
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Informed consent: Not applicable.
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Author contributions: All authors have accepted responsibility for the entire content of this manuscript and approved its submission. Neela M. Bhatia: Data curation; Formal analysis; Methodology; Project administration; Resources; Roles/Writing-original draft; Ashwini Shekhar: Investigation; Methodology; Resources; Validation; Roles/Writing–original draft. Pallavi Mane: Investigation; Methodology; Resources; Validation; Roles/Writing–original draft. Manish S. Bhatia: Conceptualization; Methodology; Project administration; Resources; Software; Supervision; Validation; Writing–review & editing. Vinod L. Gaikwad: Methodology; Project administration; Resources; Software; Validation; Writing–review & editing.
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Use of Large Language Models, AI and Machine Learning Tools: None declared.
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Conflict of interest: The authors state no conflict of interest.
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Research funding: None declared.
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Data availability: The authors confirm that the data supporting the findings of this study are available within the article.
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Supplementary Material
This article contains supplementary material (https://doi.org/10.1515/tsd-2024-2650).
© 2025 Walter de Gruyter GmbH, Berlin/Boston
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- Frontmatter
- Review Article
- Precision-engineered nanomaterials: unlocking the potential of water-in-oil microemulsions for the controlled synthesis, morphology design, and future innovations
- Micellar Catalysis
- Oxidation of l-tyrosine by diperiodatocuprate(III) in CPC micellar medium, facilitated by Ru(III)
- A comprehensive spectral study of dye-surfactant complex formation by Xylenol Orange with selective aqueous micellar media of CPC, rhamnolipids and saponin
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