Development of a new delivery system consisting in “drug – in cyclodextrin – in nanostructured lipid carriers” for ketoprofen topical delivery

Cirri, Marzia; Bragagni, Marco; Mennini, Natascia; Mura, Paola

doi:10.1016/j.ejpb.2011.07.015

Cited by 130 publications

(57 citation statements)

References 35 publications

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“…[8][9][10] The measurements were made compared with the medium of examination, methanol. Control experiments were performed using NPs without KP.…”

Section: Drug Loading (%Dl) Assessmentmentioning

confidence: 99%

“…5 It is well known that polymeric nanocarriers can improve the stability of the drug loaded, provide increased capacity for hydrophobic drug dissolution, improve bioavailability and ensure controlled release in the target biological tissues. [6][7][8][9][10] For example, pomegranate seed oil nanoemulsions containing KP and stabilized by pullulan as a polymeric emulsifier, can improve drug photostability and have better drug solubility. 7 In another study, stable KP-loaded chitosan (CH) microparticles were obtained, and the drug content was found to be more than 97.5% at the end of the first month in accelerated conditions.…”

Section: Ketoprofen ([Rs]2-[3-benzoylphenyl]-propionic Acid) (Kp) Is mentioning

confidence: 99%

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Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

Andonova¹,

Peneva²,

Georgiev³

et al. 2017

IJN

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The purpose of the study was to investigate the stability and biopharmaceutical characteristics of ketoprofen, loaded in polymeric carriers, which were included into a bigel in a semisolid dosage form. The polymer carriers with in situ-included ketoprofen were obtained by emulsifier-free emulsion polymerization of the monomers in aqueous medium or a solution of the polymers used. The morphological characteristics of the carriers, the in vitro release and the photochemical stability of ketoprofen were evaluated. The model with optimal characteristics was included in a bigel formulation. The bigel was characterized in terms of pH, rheological behavior, spreadability, and in vitro drug release. Acute skin toxicity, antinociceptive activity, anti-inflammatory activity, and antihyperalgesic effects of the prepared bigel with ketoprofen-loaded polymer carrier were evaluated. The carriers of ketoprofen were characterized by a high yield and drug loading. The particle size distribution varied widely according to the polymer used, and a sustained release was provided for up to 6 hours. The polymer mixture poly(vinyl acetate) and hydroxypropyl cellulose as a drug carrier, alone or included in the bigel composition, improved the photostability of the drug compared with unprotected ketoprofen. The bigel with ketoprofen-loaded particles provided sustained release of the drug and had optimal rheological parameters. In vivo experiments on the bigel showed no skin inflammation or irritation. Four hours after its application, a well-defined analgesic, anti-inflammatory, and antihyperalgesic effect was registered. The polymer mixture of poly(vinyl acetate) and hydroxypropyl cellulose as a carrier of ketoprofen and the bigel in which it was included provided an enhanced photostability and sustained drug release.

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“…[8][9][10] The measurements were made compared with the medium of examination, methanol. Control experiments were performed using NPs without KP.…”

Section: Drug Loading (%Dl) Assessmentmentioning

confidence: 99%

Section: Ketoprofen ([Rs]2-[3-benzoylphenyl]-propionic Acid) (Kp) Is mentioning

confidence: 99%

Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

Andonova¹,

Peneva²,

Georgiev³

et al. 2017

IJN

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“…The lipid materials used for SLNs are biodegradable and biocompatible and provide better safety profile. 10,11 Nanostructured lipid carriers (NLCs) are the second generation of SLNs and offer many advantages over SLNs. The solid lipid, when used alone for preparing SLNs, forms a perfect crystal lattice with limited space for accommodating the drugs.…”

Section: Introductionmentioning

confidence: 99%

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Rajinikanth¹,

Chellian²

2016

IJN

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The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol ® ATO 5 (glyceryl palmitostearate) and Labrasol ® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol ® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol ® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, −21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 μg/cm 2 /h) as compared with plain 5-FU gel (2.85±1.12 μg/cm 2 /h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 μg/cm 2 ) as compared with that from the 5-FU plain gel (12.23±3.86 μg/cm 2 ) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations.

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“…NLC merupakan sistem penghantaran obat yang terdiri dari campuran lipid padat dan lipid cair, membentuk matrik inti lipid yang distabilkan oleh surfaktan (Cirri, et al, 2012). Ukuran partikel NLC pada rentang 10-1000 nm (Pardeike, et al, 2009;Souto & Muller, 2007;Muller, et al, 2002).…”

Section: Meloxicam Merupakan Golonganunclassified

Pengembangan Sistem Nanostructured Lipid Carriers (NLC) Meloxicam dengan Lipid Monostearin dan Miglyol 808 Menggunakan Metode Emulsifikasi

Annisa

Hendradi

Melani

2016

J. Trop. Pharm. Chem.

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Development of a new delivery system consisting in “drug – in cyclodextrin – in nanostructured lipid carriers” for ketoprofen topical delivery

Cited by 130 publications

References 35 publications

Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

Ketoprofen-loaded polymer carriers in bigel formulation: an approach to enhancing drug photostability in topical application forms

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Pengembangan Sistem Nanostructured Lipid Carriers (NLC) Meloxicam dengan Lipid Monostearin dan Miglyol 808 Menggunakan Metode Emulsifikasi

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