Novel dual-reverse thermosensitive solid lipid nanoparticle-loaded hydrogel for rectal administration of flurbiprofen with improved bioavailability and reduced initial burst effect

Din, Fakhar ud; Mustapha, Omer; Kim, Dong Wuk; Rashid, Rehmana; Park, Jong Hyuck; Choi, Jae Young; Ku, Sae Kwang; Yong, Chul Soon; Kim, Jong Oh; Choi, Han‐Gon

doi:10.1016/j.ejpb.2015.04.019

Cited by 116 publications

(50 citation statements)

References 37 publications

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“…Our results suggested that the lipophilic solid SLN was surrounded by the hydrophilic poloxamer aqueous solution due to interfacial phenomenon, leading to the production of the DRTN system. Its excellent stability might be contributed by adequate amount of surfactants, including poloxamer, Tween 80 and Span 80 (Din et al, 2015a). However, at 36.5 C, it became foggy and round-shaped particle with slightly larger size compared to that at 25 C, suggesting that it was converted from solid to liquid form ( Figure 2D).…”

Section: Physicochemical Characterizationmentioning

confidence: 99%

“…At all times, the DRTN gave significantly lower dissolution rate of irinotecan compared to the hydrogel, and thus sustaining the release for 1 h . The DRTN could doubly regulate the discharge of the drug, first from the thermosensitive SLN and then from the thermosensitive hydrogel, leading to impeded drug dissolution and initial burst effect, and sustained release (Din et al, 2015a).…”

Section: Physicochemical Characterizationmentioning

confidence: 99%

“…The DRTN was manufactured with drug-encapsulated SLN and poloxamer solution, such that the former, were homogenously dispersed in the latter (Din et al, 2015a). It was destined that the solid form of the former and liquid form of the latter persisted at room temperature; on the contrary, the former melted to liquid and the latter altered to gel form in the body (Figure 1).…”

Section: Physicochemical Characterizationmentioning

confidence: 99%

“…The DRTN was a dispersed hydrogel system in which the thermosensitive irinotecan-encapsulated solid lipid nanoparticles (SLN) were homogenously suspended within the thermosensitive poloxamer solution. In this DRTN system, the solid form of the former and liquid form of the latter persisted at 25 C; however, the former melted to liquid and the latter altered to gel form at 36.5 C (Din et al, 2015a). Its gel properties and dissolution were investigated.…”

Section: Introductionmentioning

confidence: 99%

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Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration

et al. 2017

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Republic of Korea AbstractIntravenously administered for the treatment of rectum cancer, irinotecan produces severe side effects due to very high plasma concentrations. A novel irinotecan-encapsulated double reverse thermosensitive nanocarrier system (DRTN) for rectal administration was developed as an alternative. The DRTN was fabricated by dispersing the thermosensitive irinotecanencapsulated solid lipid nanoparticles (SLN) in the thermosensitive poloxamer solution. Its gel properties, pharmacokinetics, morphology, anticancer activity and immunohistopathology were assessed after its rectal administration to rats and tumor-bearing mice. In the DRTN, the solid form of the SLN and the liquid form of the poloxamer solution persisted at 25 C; the former melted to liquid, and the latter altered to gel at 36.5 C. The DRTN was easily administered to the anus, gelling rapidly and strongly after rectal administration. Compared to the conventional hydrogel and intravenously administered solution, it retarded dissolution and initial plasma concentration. The DRTN gave sustained release and nearly constant plasma concentrations of irinotecan at 1-3 h in rats, resulting in improved anticancer activity. It induced no damage to the rat rectum and no body weight loss in tumor-bearing mice. Thus, this irinotecan-encapsulated DRTN associated with a reduced burst effect, lack of toxicity and excellent antitumor efficacy would be strongly recommended as a rectal pharmaceutical product alternative to commercial intravenous injection in the treatment of rectum and colon cancer. KeywordsIrinotecan, double reverse thermosensitive nanocarrier, rectal administration, burst effect, toxicity, anti-tumor efficacy History

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Section: Physicochemical Characterizationmentioning

confidence: 99%

Section: Physicochemical Characterizationmentioning

confidence: 99%

Section: Physicochemical Characterizationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Irinotecan-encapsulated double-reverse thermosensitive nanocarrier system for rectal administration

et al. 2017

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“…In latter case, the formulation was first thermostated at 37 °C in suppository moulds to achieve solidification of the formulation prior its placing into basket [28]. Another approach, where a liquid suppository formulation was directly introduced into the basket covered with gauze, was also described [29]. Compendial monographs, USP Dissolution Database and FDA Dissolution Database also recommend the use of basket apparatus, both in standard and the small-volume configuration, for the in vitro testing of mucosal delivery systems (Table 1).…”

Section: Basket Apparatusmentioning

confidence: 99%