Colon-specific tablets containing 5-fluorouracil microsponges for colon cancer targeting

Othman, Mahmoud H.; Zayed, Gamal; Ali, Usama F; Abdellatif, Ahmed A. H.

doi:10.1080/03639045.2020.1844730

Cited by 18 publications

(4 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Besides topical drug delivery, a microsponge delivery system was investigated for colon targeted drug delivery systems earlier, dispensing in capsule [1] and tablet [2]. In previous years, researchers prepared and characterised microsponges entrapping various types of drugs, such as 5 -FU [3,4]; antifungal drugs-ketoconazole, miconazole, fluconazole, terbinafin HCl [5][6][7], antihypertensive drugs-nebivolol, valsartan [8,9], an anti-inflammatory drugketoprofen [10], timolol, used for glaucoma [11], antiviral drugs-valcyclovir, acyclovir [12,13], anthelmintic drug-albendazole [14].…”

Section: Introductionmentioning

confidence: 99%

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Halder

Poddar²,

Khanam

2021

Preprint

View full text Add to dashboard Cite

The present investigation aims at developing models by response surface methodology (FCCCD) followed by the scale-up method in preparing control release microsponge particles loaded with 5- fluorouracil, a drug used to treat actinic keratosis and colon cancer, and producing a new Dermal Delivery System. The polymer-based (ethyl cellulose and eudragit RS 100) microsponge particles were prepared by the w/o/w double emulsification method. The optimized product was formed with the combination of independent variables levels: polymer (600 mg), stirring speed (1198 rpm) and surfactant (2% w/v), yielding responses as yield (~63.6257%), the average size of particles (~151.563 µm), entrapment efficiency (~75.319 %) and drug release in 8hr (~75.75%), with desirability value of 0.737. The products showed similar responses as obtained in scale-up work. FT-IR, DSC and SEM studies confirmed the drug's compatibility with polymers and porous morphology. Finally, gel embedded optimised product showed shear-thinning rheological property, ideal for drug release from the thixotropic gel.

show abstract

Section: Introductionmentioning

confidence: 99%

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Halder

Poddar²,

Khanam

2021

Preprint

View full text Add to dashboard Cite

show abstract

“…On the other hand, Fig. 10 c shows abdominal radiographs that were taken 5 h post-dose; it is evident that the capsules start to lose their integrity and get smaller, leading to releasing of ITZ-ZNPs in the colon fluids [ 95 ]. This may be contributed to solubilization of Eudragit ® S100 coat when reaching the colon as it dissolves only in pH < 7 [ 96 ].…”

Section: Resultsmentioning

confidence: 99%

Fabrication and optimization of itraconazole-loaded zein-based nanoparticles in coated capsules as a promising colon-targeting approach pursuing opportunistic fungal infections

Adel

Fahmy

Elsayed

et al. 2023

Drug Deliv. and Transl. Res.

View full text Add to dashboard Cite

Itraconazole (ITZ), a broad-spectrum antifungal drug, was formulated into colon-targeting system aiming to treat opportunistic colonic fungal infections that commonly infect chronic inflammatory bowel diseases (IBD) patients due to immunosuppressive therapy. Antisolvent precipitation technique was employed to formulate ITZ-loaded zein nanoparticles (ITZ-ZNPs) using various zein: drug and aqueous:organic phase ratios. Central composite face-centered design (CCFD) was used for statistical analysis and optimization. The optimized formulation was composed of 5.5:1 zein:drug ratio and 9.5:1 aqueous:organic phase ratio with its observed particle size, polydispersity index, zeta potential, and entrapment efficiency of 208 ± 4.29 nm, 0.35 ± 0.04, 35.7 ± 1.65 mV, and 66.78 ± 3.89%, respectively. ITZ-ZNPs were imaged by TEM that revealed spherical core–shell structure, and DSC proved ITZ transformation from crystalline to amorphous form. FT-IR showed coupling of zein NH group with ITZ carbonyl group without affecting ITZ antifungal activity as confirmed by antifungal activity test that showed enhanced activity of ITZ-ZNPs over the pure drug. Histopathological examination and cytotoxicity tests ensured biosafety and tolerance of ITZ-ZNPs to the colon tissue. The optimized formulation was then loaded into Eudragit S100-coated capsules and both in vitro release and in vivo X-ray imaging confirmed the success of such coated capsules in protecting ITZ from the release in stomach and intestine while targeting ITZ to the colon. The study proved that ITZ-ZNPs is promising and safe nanoparticulate system that can protect ITZ throughout the GIT and targeting its release to the colon with effectual focused local action for the treatment of colon fungal infections. Graphical Abstract

show abstract

“…For determination of bulk and tapped densities, the standard cylinder and tapped densitometer (ERWEKA, type SVM, Germany), respectively, were used. Bulk and tapped densities were used for the calculation of Carr's index and Hausner's ratio [25][26]. For the determination of true density (ρ t ), xylene displacement method was used with equation (1).…”

Section: Determination Of Size Distribution Densitymentioning

confidence: 99%

Optimization of Pregelatinized Taro Boloso‐I Starch as a Direct Compression Tablet Excipient

Balla

Joseph

Belete

2023

BioMed Research International

View full text Add to dashboard Cite

Background. Tablets are still the most preferred means of drug delivery. The search for new and improved direct compression tablet excipients is an area of research focus. This is because the direct compression method overcomes the drawbacks of granulation methods of tablet production. It exempts several treatment steps associated with the granulation methods. The requirements for the powders to be directly compressible include flowability, low friction tendency, compressibility, and fast disintegration capacity. Taro Boloso-I is a new variety of Colocasia esculenta (L. Schott) yielding 67% more than a previously reported variety (Godare) in Ethiopia. This study is aimed at enhancing the flowability while keeping the compressibility and compactibility of the pregelatinized Taro Boloso-I starch. Methods. Central composite design was used for the optimization of two factors which were the temperature and duration of pregelatinization against 4 responses. The responses were angle of repose, Hausner’s ratio, Heckel’s yield pressure, and tablet breaking force. Results and Discussions. An increase in the temperature resulted in decrease in both the angle of repose and the Hausner ratio and that of time decreased angle of repose as well. The Heckel yield pressure was observed to increase with increasing levels of both temperature and time. The pregelatinized starch prepared by heating 15% slurry of Taro Boloso-I starch at the pregelatinization temperature of 66.22°C for 20 min showed desired flow property and compressibility. Conclusions. Pregelatinized Taro Boloso-I starch could be regarded as a potential direct compression excipient in terms of flowability, compressibility, and compactibility. The PGTBIS could perform better as filler and binder in direct compression tablets than the Starch 1500® in terms of compactibility.

show abstract

Colon-specific tablets containing 5-fluorouracil microsponges for colon cancer targeting

Cited by 18 publications

References 39 publications

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Fabrication and optimization of itraconazole-loaded zein-based nanoparticles in coated capsules as a promising colon-targeting approach pursuing opportunistic fungal infections

Optimization of Pregelatinized Taro Boloso‐I Starch as a Direct Compression Tablet Excipient

Contact Info

Product

Resources

About