Preparation of 5-fluorouracil-loaded poly(L-lactide-co-glycolide) wafer and evaluation ofin vitro release behavior

Lee, Jin Soo; Chae, Gang Soo; An, Tae Kun; Khang, Gil Son; Cho, Sun Hang; Lee, Hai Bang

doi:10.1007/bf03218350

Cited by 37 publications

(17 citation statements)

References 21 publications

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“…Hence, sharp peaks observed in the case of HA-PEG-PLGA-FU nanoparticles reveal that the crystalline nature of 5-FU is retained even when the drug is encapsulated in the nanoparticles. These findings are in line with those reported by Lee et al (2003).…”

Section: X-ray Diffractionsupporting

confidence: 94%

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Development and characterization of hyaluronic acid decorated PLGA nanoparticles for delivery of 5-fluorouracil

et al. 2010

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Section: X-ray Diffractionsupporting

confidence: 94%

“…Plain 5-FU showed an exothermic peak at 285°C, as already reported . These findings are in line with those reported by Luo et al (2000) and Lee et al (2003).…”

Section: Differential Scanning Calorimetrysupporting

confidence: 93%

Development and characterization of hyaluronic acid decorated PLGA nanoparticles for delivery of 5-fluorouracil

et al. 2010

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“…The extrapolated onset temperature in thermograms denotes the temperature at which the weight loss begins. The extrapolated onset temperature of 5-FU is 286.9 o C. The DSC thermogram of the pure 5-FU also showed a sharp melting endotherm peak at approximately 286.9 °C followed by decomposition, which was in agreement with those reported previously (Lee et al, 2003). The red curve is the % weight loss curve and it indicated that % Weight loss occurs in one step with 90% decomposition of the drug between 280 °C to 350 °C.…”

supporting

confidence: 90%

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

Gupta¹,

Tiwari²,

Tiwari³

et al. 2015

Braz. J. Pharm. Sci.

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The work was aimed at developing novel enteric coated HPMC capsules (ECHC) plugged with 5 Florouracil (5-FU) loaded Microsponges in combination with calcium pectinate beads. Modified quasiemulsion solvent diffusion method was used to formulate microsponges based on 3 2 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content) on the dependent variables (Particle size, %EE & % CDR) were determined. The optimized microsponges (F4) were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100) and/ or Eudrgit S 100 (Ed-S 100) in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h). Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer. O trabalho teve como objetivo o desenvolvimento de novas cápsulas com revestimento entérico HPMC (ECHC) conectadas com microesponjas carregadas com fluoruracila (5-FU) em combinação com grânuos de pectinato de cálcio. O método de difusão de solvente modificado quasi-emulsão foi usado para formular microesponjas com base no planejamento fatorial 3 2 e determinaram-se os efeitos das variáveis independentes (volume de solvente orgânico e conteúdo Eudragit RS100) sobre as variáveis dependentes (tamanho de partícula, EE% e % CDR). As microesponjas otimizadas (F4) foram caracterizadas por SEM, PXRD, TGA e ligadas aos grânulos de pectinato de cálcio em cápsulas de HPMC e estas foram, ainda, revestidas com polímero entérico Eudragit L 100 (Ed-L100) e/ou Eudrgit S 100 (Ed S 100) em diferentes proporções. No estudo de liberação in vitro de ECHC foi realizada em vários meios de liberação sequencial SGF durante 2 h, seguido de SIF para as próximas 6 h, e, em seguida, em SCF (na presença e na ausência de enzima pectinase por mais 16 h). A liberação do fármaco foi retardada em revestimento com a EDS-100, em comparação com mistura de EDS-100: EDL-100, de revestimento. O percentual de 5-FU liberado de ECHC 3 ao final de 24 h foi 97,83 ± 0,12% em presença de pectinase, enquanto...

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“…The total amount of drug released was similar for PCL/FU tablets manufactured using the lower and higher laser powers and are associated with small differences presented by both condition in the sintering degree and porosity. This drug release pattern is very common with FU polymeric drug delivery systems and has been reported by many researchers [31][32][33]. The initial amount of FU released by the sintered PCL/FU tablets is a desirable profile to provide a high initial concentration of the drug locally in the cancer cells following implantation.…”

Section: Resultsmentioning

confidence: 63%

3D printing of PCL/Fluorouracil tablets by selective laser sintering: Properties of implantable drug delivery for cartilage cancer treatment

Gv¹,

Fe²,

Gb³

et al. 2017

Rheumatol Orthop Med

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In this study, implantable polycaprolactone/fluorouracil tablets were additively manufactured by selective laser sintering using different laser power levels. PCL/FU tablets showed on SEM-EDS small particles of fluorouracil dispersed on the surface and into the porous PCL matrix. The crystallinity values for the PCL/FU tablets were lower than for the pure PCL tablets, probably due to interaction of the FU particles with the polymer chains during the solidification process. The PCL/FU tablets prepared using the higher laser power (7 W) had the highest flexural modulus, probably due to better PCL particle coalescence, higher sinter degree and the dispersion of FU particles in the co-continuous porous PCL matrix. Initially the PCL/FU tablets provided a rapid release of a high concentration of the drug at the site of the cancer cells and a subsequent controlled release sustaining levels of the chemotherapeutic agent in the region of the tumor. This 2-stage release of the drug can be a desirable profile in cartilage cancer treatment.

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Preparation of 5-fluorouracil-loaded poly(L-lactide-co-glycolide) wafer and evaluation ofin vitro release behavior

Cited by 37 publications

References 21 publications

Development and characterization of hyaluronic acid decorated PLGA nanoparticles for delivery of 5-fluorouracil

Development and characterization of hyaluronic acid decorated PLGA nanoparticles for delivery of 5-fluorouracil

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

3D printing of PCL/Fluorouracil tablets by selective laser sintering: Properties of implantable drug delivery for cartilage cancer treatment

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