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Revisiting the nanoformulation design approach for effective delivery of topotecan in its stable form: an appraisal of its in vitro Behavior and tumor amelioration potential
- Source :
- Drug Delivery. 23:2827-2837
- Publication Year :
- 2015
- Publisher :
- Informa UK Limited, 2015.
-
Abstract
- Topotecan (TPT) is indicated against a variety of solid tumors, but has restricted clinical use owing to associated pharmaceutical caveats. This study is focused at formulating a successful TPT PLGA nanosystem which ameliorates the rapid conversion of active lactone form of drug to its inactive carboxylate form and consequently improvises its efficacy. TPT PLGA nanoparticles were formulated by a double emulsion-solvent evaporation technique with sequential optimization to obtain desired particle size, PDI, zeta potential, and entrapment efficiency. Stability of TPT was ensured by maintaining an acidic pH in the drug-containing phase and the system was evaluated for in vitro-in vivo performance including cytotoxic potency. The optimized nanosystem had a particle size of 187.33 ± 7.50 nm, a PDI of 0.179 ± 0.05, and an entrapment efficiency of 56 ± 1.2%. Low pH in the interior of nanoparticles stabilized the drug to remain in its active lactone form and revealed a biphasic release pattern till 15 d. Additionally, an in vitro cytotoxicity testing as well as in vivo antitumor efficacy demonstrated a significant potential of higher proliferation inhibition as compared with neat drug (TPT). Thus, the investigation summarized an innovative simple tool for developing stable TPT NPs for effective delivery for treating solid tumors.
- Subjects :
- Drug
Chemistry, Pharmaceutical
media_common.quotation_subject
Pharmaceutical Science
Nanoparticle
02 engineering and technology
Pharmacology
Mice
03 medical and health sciences
chemistry.chemical_compound
Drug Delivery Systems
0302 clinical medicine
In vivo
Cell Line, Tumor
Neoplasms
Zeta potential
medicine
Animals
Particle Size
Cytotoxicity
media_common
Drug Carriers
Chemistry
General Medicine
021001 nanoscience & nanotechnology
PLGA
030220 oncology & carcinogenesis
Biophysics
Nanoparticles
Emulsions
Topotecan
Particle size
0210 nano-technology
medicine.drug
Subjects
Details
- ISSN :
- 15210464 and 10717544
- Volume :
- 23
- Database :
- OpenAIRE
- Journal :
- Drug Delivery
- Accession number :
- edsair.doi.dedup.....09d95689108e8134774b45055fbec5e8