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pH-and thermo-sensitive pluronic/poly(acrylic acid) in situ hydrogels for sustained release of an anticancer drug.
J Drug Target. 2013 Jan; 21(1):54-66.JD

Abstract

In this study, we developed oral in situ gelling formulations composed of pluronic (Plu) and polyacrylic acid (PAA) for the delivery of an anticancer drug, epirubicin (Epi). We investigated various Plu/PAA/Epi formulations for their physicochemical properties and in vitro permeation and accumulation, as well as for in vivo pharmacokinetic and antitumor efficacy. A scanning electron microscopic (SEM) image of Plu 14%/PAA 0.75%/Epi hydrogel showed a sponge-like structure. This formulation has suitable gelation time, water content, bioadhesive force, structural stability, and a high permeation percentage of Epi, with sustained drug release characteristics for 96 h. This hydrogel was retained at the end of the ileum near the colon of Sprague-Dawley (SD) rats for at least 12 h. An in vivo pharmacokinetic study using SD rats showed that after oral administration in this formulation, Epi had prolonged half-life, greater area under the curve, and higher relative bioavailability than in an oral Epi solution. In vivo tumor growth inhibition of Epi in this formulation was more pronounced compared with oral Epi and intravenous Epi solutions in CT-26 mouse colon adenocarcinoma bearing Balb/c mice. This study highlights the advantages of using oral in situ temperature- and pH-sensitive hydrogels for future cancer therapy.

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Authors+Show Affiliations

Lo YL
Department of Biological Sciences and Technology, National University of Tainan, Tainan, Taiwan. yulilo@mail.nutn.edu.tw
Hsu CY
No affiliation info available
Lin HR
No affiliation info available

MeSH

Acrylic ResinsAdenocarcinomaAdministration, OralAnimalsAntibiotics, AntineoplasticArea Under CurveBiological AvailabilityColonic NeoplasmsDelayed-Action PreparationsDrug CarriersDrug Delivery SystemsEpirubicinHalf-LifeHydrogelsHydrogen-Ion ConcentrationMaleMiceMice, Inbred BALB CMice, NudeMicroscopy, Electron, ScanningPoloxamerRatsRats, Sprague-DawleyTemperature

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23009351

Citation

Lo, Yu-Li, et al. "PH-and Thermo-sensitive Pluronic/poly(acrylic Acid) in Situ Hydrogels for Sustained Release of an Anticancer Drug." Journal of Drug Targeting, vol. 21, no. 1, 2013, pp. 54-66.
Lo YL, Hsu CY, Lin HR. PH-and thermo-sensitive pluronic/poly(acrylic acid) in situ hydrogels for sustained release of an anticancer drug. J Drug Target. 2013;21(1):54-66.
Lo, Y. L., Hsu, C. Y., & Lin, H. R. (2013). PH-and thermo-sensitive pluronic/poly(acrylic acid) in situ hydrogels for sustained release of an anticancer drug. Journal of Drug Targeting, 21(1), 54-66. https://doi.org/10.3109/1061186X.2012.725406
Lo YL, Hsu CY, Lin HR. PH-and Thermo-sensitive Pluronic/poly(acrylic Acid) in Situ Hydrogels for Sustained Release of an Anticancer Drug. J Drug Target. 2013;21(1):54-66. PubMed PMID: 23009351.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - pH-and thermo-sensitive pluronic/poly(acrylic acid) in situ hydrogels for sustained release of an anticancer drug. AU - Lo,Yu-Li, AU - Hsu,Chin-Yu, AU - Lin,Hong-Ru, Y1 - 2012/09/26/ PY - 2012/9/27/entrez PY - 2012/9/27/pubmed PY - 2013/6/12/medline SP - 54 EP - 66 JF - Journal of drug targeting JO - J Drug Target VL - 21 IS - 1 N2 - In this study, we developed oral in situ gelling formulations composed of pluronic (Plu) and polyacrylic acid (PAA) for the delivery of an anticancer drug, epirubicin (Epi). We investigated various Plu/PAA/Epi formulations for their physicochemical properties and in vitro permeation and accumulation, as well as for in vivo pharmacokinetic and antitumor efficacy. A scanning electron microscopic (SEM) image of Plu 14%/PAA 0.75%/Epi hydrogel showed a sponge-like structure. This formulation has suitable gelation time, water content, bioadhesive force, structural stability, and a high permeation percentage of Epi, with sustained drug release characteristics for 96 h. This hydrogel was retained at the end of the ileum near the colon of Sprague-Dawley (SD) rats for at least 12 h. An in vivo pharmacokinetic study using SD rats showed that after oral administration in this formulation, Epi had prolonged half-life, greater area under the curve, and higher relative bioavailability than in an oral Epi solution. In vivo tumor growth inhibition of Epi in this formulation was more pronounced compared with oral Epi and intravenous Epi solutions in CT-26 mouse colon adenocarcinoma bearing Balb/c mice. This study highlights the advantages of using oral in situ temperature- and pH-sensitive hydrogels for future cancer therapy. SN - 1029-2330 UR - https://www.unboundmedicine.com/medline/citation/23009351/pH_and_thermo_sensitive_pluronic/poly_acrylic_acid__in_situ_hydrogels_for_sustained_release_of_an_anticancer_drug_ L2 - https://www.tandfonline.com/doi/full/10.3109/1061186X.2012.725406 DB - PRIME DP - Unbound Medicine ER -