Preparation and in vitro characterization of SN-38-loaded, self-forming polymeric depots as an injectable drug delivery system

Manaspon, Chawan; Hongeng, Suradej; Boongird, Atthaporn; Nasongkla, Norased

doi:10.1002/jps.23238

Cited by 18 publications

(22 citation statements)

References 34 publications

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“…Injectable polymeric depots encapsulating SN38 have been prepared from copolymers synthesised with different ratios of D,L-lactide (LA), ε-caprolactone (CL) and PEG [111]. SN38 loading in the polymeric depots was dependent on the ratio between LA and CL, and up to 30% (w/w) drug loading with entrapment efficiency of more than 98% was achieved with the optimised depot formulation.…”

Section: Polymeric Depotsmentioning

confidence: 99%

Prodrug and nanomedicine approaches for the delivery of the camptothecin analogue SN38

Bala

Rao

Boyd

et al. 2013

Journal of Controlled Release

173

131

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Section: Polymeric Depotsmentioning

confidence: 99%

Prodrug and nanomedicine approaches for the delivery of the camptothecin analogue SN38

Bala

Rao

Boyd

et al. 2013

Journal of Controlled Release

173

131

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“…They have been shown to be successful in delivering a diverse range of therapeutic agents, including local chemotherapeutics for intratumoral cancer treatment [1–5], doxycycline for the treatment of periodontal disease[6, 7], and sucrose acetate isobutyrate for the treatment of schizophrenia and bipolar disorder[8]. Phase-sensitive ISFIs, first patented by Dunn et al in 1990, are made from a hydrolytically degradable and water insoluble polymer that is co-dissolved with a therapeutic agent in a water miscible organic solvent[9, 10].…”

Section: Introductionmentioning

confidence: 99%

Macroporous acrylamide phantoms improve prediction of in vivo performance of in situ forming implants

Hernandez

Gawlik

Goss

et al. 2016

Journal of Controlled Release

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In situ forming implants (ISFIs) have shown promise as a sustained, local drug delivery system for therapeutics in a variety of applications. However, development of ISFIs has been hindered by poor correlation between in vitro study results and in vivo performance. In contrast to oral dosage forms, there is currently no clear consensus on a standard for in vitro drug dissolution studies for parenteral formulations. Recent studies have suggested that the disparity between in vivo and in vitro behavior of phase-inverting ISFIs may be, in part, due to differences in injection site stiffness. Accordingly, this study aimed to create acrylamide-based hydrogel phantoms of various porosities and stiffness, which we hypothesized would better predict in vivo performance. Implant microstructure and shape were found to be dependent on the stiffness of the phantoms, while drug release was found to be dependent on both phantom porosity and stiffness. Specifically, SEM analysis revealed that implant porosity and interconnectivity decreased with increasing phantom stiffness and better mimicked the microstructure seen in vivo. Burst release of drug increased from 31% to 43% when in standard acrylamide phantoms vs macroporous phantoms (10 kPa), improving the correlation to the burst release seen in vivo. Implants in 30 kPa macroporous phantoms had the best correlation with in vivo burst release, significantly improving (p < 0.05) the burst release relative to in vivo from 64%, using a standard PBS dissolution method, to 92%. These findings confirm that implant behavior is affected by injection site stiffness. Importantly, with appropriate optimization and validation, hydrogel phantoms such as the one investigated here could be used to improve the in vitro-in vivo correlation of in situ forming implant formulations and potentially augment their advancement to clinical use.

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“…29 Additionally, polymeric depots system could provide a protection for encapsulated drug and maintain it activated along the release period. 18 Tumors that received double injections at high dose showed significantly smaller tumor volume than the other groups. Moreover, its normalized area of cell death was the highest.…”

Section: Sn-38 Distribution In Tumorsmentioning

confidence: 96%

“…38 in tumor tissues could be calculated in the range of 0.10-0.27 mg after in vivo release 18. Results mentioned above led to the significant tumor suppression effect of double injections at high dose.…”

mentioning

confidence: 90%

Antitumor efficacy and intratumoral distribution of SN-38 from polymeric depots in brain tumor model

Vejjasilpa

Nasongkla

Manaspon

et al. 2015

Exp Biol Med (Maywood)

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We investigate antitumor efficacy and 2D and 3D intratumoral distribution of 7-ethyl-10-hydroxycamptothecin (SN-38) from polymeric depots inside U-87MG xenograft tumor model in nude mice. Results showed that polymeric depots could be used to administer and controlled release of a large amount of SN-38 directly to the brain tumor model. SN-38 released from depots suppressed tumor growth, where the extent of suppression greatly depended on doses and the number of depot injections. Tumor suppression of SN-38 from depots was three-fold higher in animals which received double injections of depots at high dose (9.7 mg of SN-38) compared to single injection (2.2 mg). H&E staining of tumor sections showed that the area of tumor cell death/survival of the former group was two-fold higher than those of the latter group. Fluorescence imaging based on self-fluorescent property of SN-38 was used to evaluate the intratumoral distribution of this drug compared to histological results. The linear correlation between fluorescence intensity and the amount of SN-38 allowed quantitative determination of SN-38 in tumor tissues. Results clearly showed direct correlation between the amount of SN-38 in tumor sections and cancer cell death. Moreover, 3D reconstruction representing the distribution of SN-38 in tumors was obtained. Results from this study suggest the rationale for intratumoral drug administration and release of drugs inside tumor, which is necessary to design drug delivery systems with efficient antitumor activity.

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Preparation and in vitro characterization of SN-38-loaded, self-forming polymeric depots as an injectable drug delivery system

Cited by 18 publications

References 34 publications

Prodrug and nanomedicine approaches for the delivery of the camptothecin analogue SN38

Prodrug and nanomedicine approaches for the delivery of the camptothecin analogue SN38

Macroporous acrylamide phantoms improve prediction of in vivo performance of in situ forming implants

Antitumor efficacy and intratumoral distribution of SN-38 from polymeric depots in brain tumor model

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