Design and application of oral colon administration system

Cheng, Hao; Huang, Shiyu; Huang, Gangliang

doi:10.1080/14756366.2019.1655406

Cited by 20 publications

(9 citation statements)

References 59 publications

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“…[ 27 ] Thus, they represent a viable alternative to enteric coatings which have to pass the stomach and will have a considerably longer time until the biological action sets in. [ 1a,2a,32 ] Together with reports on the rectal delivery of drugs by suppositories, [ 3,16b,16c,17b ] it was shown here that it is possible to transport bioactive nanoparticles with probably high patient compliance. Of course, a transfection or a gene silencing as examples for gene therapy are different from a conventional drug delivery, but it may be predicted that the fatty environment inside the suppository is protecting the nanoparticles from external degradation by nucleases.…”

Section: Resultssupporting

confidence: 56%

Suppositories with bioactive calcium phosphate nanoparticles for intestinal transfection and gene silencing

Hosseini

Epple

2020

Nano Select

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Calcium phosphate nanoparticles (diameter about 60 nm, triple‐shell) were loaded with nucleic acids (DNA or siRNA) for local gene therapy in the colon. To avoid the oral administration where a passage through the stomach is necessary, the nanoparticles were incorporated into custom‐made hard‐fat suppositories after freeze‐drying with trehalose. After melting the suppository at 37°C, the nanoparticles were released and well dispersed in cell culture medium. They retained their bioactivity as shown by in vitro cell culture studies with the model cell line HeLa and the colon cancer cell line Caco‐2. The nanoparticles were easily taken up by both cell types and also efficient for transfection and gene silencing, as shown with the model protein eGFP. This opens a way for local gene therapy in the colon.

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Section: Resultssupporting

confidence: 56%

Suppositories with bioactive calcium phosphate nanoparticles for intestinal transfection and gene silencing

Hosseini

Epple

2020

Nano Select

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“…In contrast, the coated capsules showed rapid release of particles within 90 min at pH 7.1, i.e., under the neutral conditions in the colon ( Figure 6 and Figure 7 ). As passage from the stomach to the colon takes hours [ 7 , 82 , 83 , 84 , 85 ], this release rate is well suited to transporting particles to the colon.…”

Section: Resultsmentioning

confidence: 99%

Pathways for Oral and Rectal Delivery of Gold Nanoparticles (1.7 nm) and Gold Nanoclusters into the Colon: Enteric-Coated Capsules and Suppositories

et al. 2021

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Two ways to deliver ultrasmall gold nanoparticles and gold-bovine serum albumin (BSA) nanoclusters to the colon were developed. First, oral administration is possible by incorporation into gelatin capsules that were coated with an enteric polymer. These permit the transfer across the stomach whose acidic environment damages many drugs. The enteric coating dissolves due to the neutral pH of the colon and releases the capsule’s cargo. Second, rectal administration is possible by incorporation into hard-fat suppositories that melt in the colon and then release the nanocarriers. The feasibility of the two concepts was demonstrated by in-vitro release studies and cell culture studies that showed the easy redispersibility after dissolution of the respective transport system. This clears a pathway for therapeutic applications of drug-loaded nanoparticles to address colon diseases, such as chronic inflammation and cancer.

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“…The polyelectrolytes formulation consists an effective carrier for hydrophobic molecules as ivermectin [14,16]. Indeed, both main components, i.e., chitosan and alginate have shown excellent characteristics for applications in drug delivery materials [25,26,27]. Since both macromolecules are weak polyelectrolytes, the charge balance between COO À and NH 3 þ groups, which are pH-dependent, triggers structure characteristics as well the interaction with the biological media [14,16].…”

Section: Formulation and In Vivo Administrationmentioning

confidence: 99%

Safety of oral administration of high doses of ivermectin by means of biocompatible polyelectrolytes formulation

Madrid

Mathews

Patta

et al. 2021

Heliyon

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The FDA-approved drug ivermectin is applied for treatments of onchocerciasis and lymphatic filariasis. The anticancer and anti-viral activities have been demonstrated stressing possibilities for the drug repurposing and therefore new information on high dosage safety is on demand. We analyzed in vivo tissue responses for high doses of ivermectin using Corydoras fish as animal model. We made intestinal histology and hematologic assays after oral administration of ivermectin transported with polyelectrolytes formulation. Histology showed any apparent damage of intestinal tissues at 0.22-170 mg of ivermectin/kg body weight. Immunofluorescence evidenced delocalization of Myosin-Vb at enterocytes only for the higher dose. Hematology parameters showed random variations after 7 days from administration, but a later apparent recover after 14 and 21 days. The study evaluated the potential of high doses of oral administration of ivermectin formulation, which could be an alternative with benefits in high compliance therapies.

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Design and application of oral colon administration system

Cited by 20 publications

References 59 publications

Suppositories with bioactive calcium phosphate nanoparticles for intestinal transfection and gene silencing

Suppositories with bioactive calcium phosphate nanoparticles for intestinal transfection and gene silencing

Pathways for Oral and Rectal Delivery of Gold Nanoparticles (1.7 nm) and Gold Nanoclusters into the Colon: Enteric-Coated Capsules and Suppositories

Safety of oral administration of high doses of ivermectin by means of biocompatible polyelectrolytes formulation

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