Non-uniform drug distribution matrix system (NUDDMat) for zero-order release of drugs with different solubility

Cerea, Matteo; Foppoli, Anastasia; Palugan, Luca; Melocchi, Alice; Gazzaniga, A.

doi:10.1016/j.ijpharm.2020.119217

Cited by 10 publications

(6 citation statements)

References 47 publications

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“…49 The release profiles of ATST or TAGE from ATST LNPs and TAGE ZNPs followed zero order kinetics which indicated that the drug release is independent of the drug concentration. 50 Drugs released from RGD-ATST/TAGE CNPs followed the Higuchi model, indicating drug release by diffusion. 51 Faster release of ATST was found than that of TAGE from ATST/TAGE CNPs, which could be explained by the fact that ATST was in the outer layer of the nano-system and will be released earlier.…”

Section: Discussionmentioning

confidence: 95%

<p>Synergistic Effect of Tangeretin and Atorvastatin for Colon Cancer Combination Therapy: Targeted Delivery of These Dual Drugs Using RGD Peptide Decorated Nanocarriers</p>

He¹,

Zheng

Li³

et al. 2020

DDDT

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Colorectal cancer (CRC) is the third most frequently diagnosed cancer and the fourth leading cause of cancer death over the world. Nano-sized drug delivery systems are used for the treatment of cancers. The aim of this study was to develop a tangeretin (TAGE) and atorvastatin (ATST) combined nano-system decorated with RGD (RGD-ATST/TAGE CNPs) for colon cancer combination therapy. Materials and Methods: In this study, cyclized arginine-glycine-aspartic acid sequences (RGD) contained ligand was synthesized by conjugating cyclo (Arg-Gly-Asp-d-Phe-Lys) (cRGDfK) with D-α-tocopheryl succinate dichloromethane (TOSD) using polyethylene glycol (PEG) as a linker to obtain cRGDfK-PEG-TOSD. ATST and TAGE combined nanosystems: RGD-ATST/TAGE CNPs were prepared. The combination effects as well as antitumor effects of these two agents were evaluated on colon cancer cells and mice bearing cancer models. Results: Drug entrapment efficiencies of nano-systems were high (around 90%), suggesting the good loading capacity. The release profiles of ATST or TAGE from RGD-ATST/TAGE CNPs followed Higuchi model. The RGD-decorated nano-system showed more obvious cytotoxicity on HT-29 cells than the undecorated nano-system, but no obvious difference was found on normal CCD-18 cells. The strongest synergism was observed when the weight ratio of ATST to TAGE was 1:1. In vivo biodistribution of RGD-ATST/TAGE CNPs in the tumor site is high and prominently inhibited the in vivo tumor growth. Conclusion: The results demonstrated that RGD-ATST/TAGE CNPs showed the most significant synergistic therapeutic efficacy, exhibited no significant toxicity to major organs and tissues, and body weight of the treated mice was stable. Therefore, the combination nano-system is a promising platform for colon cancer therapy.

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Section: Discussionmentioning

confidence: 95%

<p>Synergistic Effect of Tangeretin and Atorvastatin for Colon Cancer Combination Therapy: Targeted Delivery of These Dual Drugs Using RGD Peptide Decorated Nanocarriers</p>

He¹,

Zheng

Li³

et al. 2020

DDDT

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“…J o u r n a l P r e -p r o o f A novel drug delivery system with non-uniform distribution of drug, the Non-Uniform Drug Distribution Matrix (NUDDMat), was recently developed [74,75]. The system was prepared by powder-layering technique, i.e.…”

Section: Multilayered Drug-coated Granulesmentioning

confidence: 99%

Oral hydrophilic matrices having non uniform drug distribution for zero-order release: A literature review

Cerea

Maroni

Palugan

et al. 2020

Journal of Controlled Release

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“…Recently, powder-layering technique has been proposed for the application of time-dependent functional coatings based on HPMC [ 5 , 44 ]. This technique, which has been developed for loading active pharmaceutical ingredients in powder form onto inert cores, consists in the addition of powders and of a binding formulation in alternating or simultaneous mode inside the process chamber of the coating equipment, where the substrates are properly fluidized [ 45 ]. The powders adhere to the wet cores, and, due to liquid inter-particle bonds turning into solid structures after solvent evaporation, ultimately form a coherent layer.…”

Section: Introductionmentioning

confidence: 99%

Colon Drug Delivery Systems Based on Swellable and Microbially Degradable High-Methoxyl Pectin: Coating Process and In Vitro Performance

Moutaharrik,

Palugan,

Cerea

et al. 2024

Pharmaceutics

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Oral colon delivery systems based on a dual targeting strategy, harnessing time- and microbiota-dependent release mechanisms, were designed in the form of a drug-containing core, a swellable/biodegradable polysaccharide inner layer and a gastroresistant outer film. High-methoxyl pectin was employed as the functional coating polymer and was applied by spray-coating or powder-layering. Stratification of pectin powder required the use of low-viscosity hydroxypropyl methylcellulose in water solution as the binder. These coatings exhibited rough surfaces and higher thicknesses than the spray-coated ones. Using a finer powder fraction improved the process outcome, coating quality and inherent barrier properties in aqueous fluids. Pulsatile release profiles and reproducible lag phases of the pursued duration were obtained from systems manufactured by both techniques. This performance was confirmed by double-coated systems, provided with a Kollicoat® MAE outer film that yielded resistance in the acidic stage of the test. Moreover, HM pectin-based coatings manufactured by powder-layering, tested in the presence of bacteria from a Crohn’s disease patient, showed earlier release, supporting the role of microbial degradation as a triggering mechanism at the target site. The overall results highlighted viable coating options and in vitro release characteristics, sparking new interest in naturally occurring pectin as a coating agent for oral colon delivery.

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Non-uniform drug distribution matrix system (NUDDMat) for zero-order release of drugs with different solubility

Cited by 10 publications

References 47 publications

<p>Synergistic Effect of Tangeretin and Atorvastatin for Colon Cancer Combination Therapy: Targeted Delivery of These Dual Drugs Using RGD Peptide Decorated Nanocarriers</p>

<p>Synergistic Effect of Tangeretin and Atorvastatin for Colon Cancer Combination Therapy: Targeted Delivery of These Dual Drugs Using RGD Peptide Decorated Nanocarriers</p>

Oral hydrophilic matrices having non uniform drug distribution for zero-order release: A literature review

Colon Drug Delivery Systems Based on Swellable and Microbially Degradable High-Methoxyl Pectin: Coating Process and In Vitro Performance

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