Cited by 79Nanoparticle-Based Drug DeliveryCurcumin's Biomedical ApplicationsAdvanced Drug Delivery Systems

Cholesterol-conjugated poly(D, L-lactide)-based micelles as a nanocarrier system for effective delivery of curcumin in cancer therapy

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Kumari, Preeti, Muddineti, Omkara Swami, Rompicharla, Sri Vishnu Kiran, Ghanta, Pratyusha, B B N, Adithya Karthik, Ghosh, Balaram, Biswas, Swati·2017·Drug Delivery

Abstract

Polymeric micelles have been widely explored preclinically as suitable delivery systems for poorly soluble chemotherapeutic drugs in cancer therapy. The present study reported the development of cholesterol (Ch)-conjugated poly(D,L-Lactide) (PLA)-based polymeric micelles (mPEG–PLA-Ch) for effective encapsulation and delivery of curcumin (CUR) at the tumor site. Cholesterol conjugation dramatically affected the particle size and improved drug loading (DL) and encapsulation efficiency (EE). mPEG–PLA-Ch-CUR showed bigger hydrodynamic diameter (104.6 ± 2.1 nm, and 169.3 ± 1.52 nm for mPEG–PLA and mPEG–PLA-Ch, respectively) due to increased size of the hydrophobic core. The newly developed polymer exhibited low critical micelles concentration (CMC) (25 μg/mL) which is close to lipid-based polymer, PEG-phosphatidyl ethanolamine (12.5 μg/mL) compared to mPEG–PLA (50 μg/mL). mPEG–PLA-Ch micelles exhibited relatively higher EE (93.74 ± 1.6%) and DL (11.86 ± 0.8%) compared to mPEG–PLA micelles (EE 91.89 ± 1.2% and DL 11.06 ± 0.8%). mPEG–PLA-Ch micelles were internalized by the cancer cells effectively and exhibited higher cytotoxicity compared to free CUR in both, murine melanoma (B16F10) and human breast cancer (MDA-MB-231) cells. mPEG–PLA-Ch exhibited satisfactory hemocompatibility indicating their potential for systemic application. Further, mPEG–PLA-Ch-CUR demonstrated higher rate of reduction of tumor volume in B16F10-xenografted tumor-bearing mice compared to free CUR. At the end of 22 days, the tumor reduced to 1.87-fold (627.72 ± 0.9 mm3 versus 1174.68 ± 1.64 mm3) compared to the treatment with free CUR. In conclusion, the experimental data in vitro and in vivo indicated that the newly developed CUR-mPEG–PLA-Ch micelles may have promising applications in solid tumors.

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Authors
Kumari, P., Muddineti, O. S., Rompicharla, S. V. K., Ghanta, P., B B N, A. K., Ghosh, B., & Biswas, S.
Affiliations
  • Birla Institute of Technology and Science, Pilani (IN)
  • Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad, India
Corresponding author
Biswas, Swati
Venue
Drug Delivery
Published
2017-01-01
Volume
24
Issue
1
Pages
209-223
ISSN
  • 1071-7544 (ISSN-L)
  • 1521-0464
OpenAlex
W2583238555
Cited by
79
References
60
Citations by year
2026: 1 · 2025: 5 · 2024: 5 · 2023: 9 · 2022: 11 · 2021: 11 · 2020: 8 · 2019: 14 · 2018: 12 · 2017: 3
FWCI
3.64
Type
journal article
Language
en
Open access
Locations
  • Drug Delivery (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Topics
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Curcumin's Biomedical Applications
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Keywords
polymeric micelles, curcumin delivery, nanocarriers, tumor targeting, encapsulation efficiency, drug loading, melanoma, breast cancer, tumor xenografts, hemocompatibility, critical micelle concentration, hydrodynamic diameter
MeSH terms
Animals, Antineoplastic Agents, Breast Neoplasms, Cholesterol, Curcumin, Drug Carriers, Female, Melanoma, Experimental, Mice, Inbred C57BL, Micelles, Particle Size, Polyesters, Polyethylene Glycols, Polymers, Cell Line, Tumor, Mice

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