Fabrication of covered porous PLGA microspheres using hydrogen peroxide for controlled drug delivery and regenerative medicine

Bae, Soon Eon; Son, Jun Sik; Park, Kwideok; Han, Dong Keun

doi:10.1016/j.jconrel.2008.09.006

Cited by 170 publications

(114 citation statements)

References 22 publications

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“…Previously described methods of microsponge preparation by quasi emulsion solvent diffusion technique Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer 593 using porogen (Bae et al, 2009;Graves et al, 2005) were modified to employ an aqueous solution of sodium chloride as porogen. 1% (w/v) aqueous solution of the porogen (NaCl) was prepared and sufficient amount of Span 80 was added to it with agitation to obtain1% (v/v) dispersion.…”

Section: Methods Development For the Fabrication Of Microspongesmentioning

confidence: 99%

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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Section: Methods Development For the Fabrication Of Microspongesmentioning

confidence: 99%

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.

View full text Add to dashboard Cite

show abstract

“…Although these studies could prevent the partitioning effect of water-soluble drugs, a large amount of excipient was required and the drug loading was low. In order to increase the capacity of drug loading in particles, alternative methods such as supercritical anti-solvent (14), electrospinning process using biodegradable polymers (15), culturing of drug into yeast cells (16), gelatin coacervation-phase separation method (17), and using hydrogen peroxide to make porous microspheres (18) have been investigated. Nevertheless, most pseudoephedrine HCl and ovalbumin at a ratio of 1:2, PEO23…”

Section: Introductionmentioning

confidence: 99%

Solubility of Drugs in Aqueous Polymeric Solution: Effect of Ovalbumin on Microencapsulation Process

2011

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Abstract. Microencapsulation of water-soluble drugs using coacervation-phase separation method is very challenging, as these drugs partitioned into the aqueous polymeric solution, resulting in poor drug entrapment. For evaluating the effect of ovalbumin on the microencapsulation of drugs with different solubility, pseudoephedrine HCl, verapamil HCl, propranolol HCl, paracetamol, and curcuminoid were used. In addition, drug mixtures comprising of paracetamol and pseudoephedrine HCl were also studied. The morphology, encapsulation efficiency, particle size, and in vitro release profile were investigated. The results showed that the solubility of the drug determined the ratio of ovalbumin to be used for successful microencapsulation. The optimum ratios of drug, ovalbumin, and gelatin for water-soluble (pseudoephedrine HCl, verapamil HCl, and propranolol HCl), sparingly water-soluble (paracetamol), and waterinsoluble (curcuminoid) drugs were found to be 1:1:2, 2:3:5, and 1:3:4. As for the drug mixture, the optimum ratio of drug, ovalbumin, and gelatin was 2:3:5. Encapsulated particles prepared at the optimum ratios showed high yield, drug loading, entrapment efficiency, and sustained release profiles. The solubility of drug affected the particle size of the encapsulated particle. Highly soluble drugs resulted in smaller particle size. In conclusion, addition of ovalbumin circumvented the partitioning effect, leading to the successful microencapsulation of water-soluble drugs.

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“…Secondly, a higher hydration rate of tricalcium silicate may lead to enhanced bonding between matrix particles by improving the agglomeration and the subsequent solidification of C-S-H gel networks. It is assumed that with the formation of macroporous structure by the decomposition of H 2 O 2 as porogen, the reactive surface for the hydration would be larger in the scaffold than in the specimen without porogen during the aging process in humidity, and such an increase in reactive surface has been figured out in a previous research on the fabrication of porous PLGA microspheres with H 2 O 2 as porogen [30]. Therefore, an accelerated hydration and resultant higher content of hydration product within the scaffold were observed from the results of XRD analysis (Fig.…”

Section: Discussionmentioning

confidence: 99%

Low-temperature fabrication of macroporous scaffolds through foaming and hydration of tricalcium silicate paste and their bioactivity

2010

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A low-temperature fabrication method for highly porous bioactive scaffolds was developed. The twostep method involved the foaming of tricalcium silicate cement paste and hydration to form calcium silicate hydrate and calcium hydroxide. Scaffolds with a combination of interconnected macro-and micro-sized pores were fabricated by making use of the decomposition of a hydrogen peroxide (H 2 O 2 ) solution that acted as a foaming agent and through the hydration of tricalcium silicate cement. It was found possible to control the porosity and pore sizes by adjusting the concentration of the H 2 O 2 solution. The in vitro bioactivity of the highly porous scaffolds was investigated by immersion in simulated body fluid (SBF) for 7 days. Hydroxyapatite (HAp) was formed on the surface of the scaffolds. Their bioactivity could be expected to be as good as that of tricalcium silicate cement, making the material competent for the bone tissue engineering application.

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Fabrication of covered porous PLGA microspheres using hydrogen peroxide for controlled drug delivery and regenerative medicine

Cited by 170 publications

References 22 publications

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

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

Solubility of Drugs in Aqueous Polymeric Solution: Effect of Ovalbumin on Microencapsulation Process

Low-temperature fabrication of macroporous scaffolds through foaming and hydration of tricalcium silicate paste and their bioactivity

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