scholarly journals Oligonucleotide Delivery across the Caco-2 Monolayer: The Design and Evaluation of Self-Emulsifying Drug Delivery Systems (SEDDS)

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 459
Author(s):  
Jana Kubackova ◽  
Ondrej Holas ◽  
Jarmila Zbytovska ◽  
Barbora Vranikova ◽  
Guanghong Zeng ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Cell Monolayer ◽  
Cationic Lipid ◽  
Delivery Systems ◽  
Promising Tool ◽  
Promising Therapeutic Approach ◽  
Oligonucleotide Delivery ◽  
Dimethyldioctadecylammonium Bromide

Oligonucleotides (OND) represent a promising therapeutic approach. However, their instability and low intestinal permeability hamper oral bioavailability. Well-established for oral delivery, self-emulsifying drug delivery systems (SEDDS) can overcome the weakness of other delivery systems such as long-term instability of nanoparticles or complicated formulation processes. Therefore, the present study aims to prepare SEDDS for delivery of a nonspecific fluorescently labeled OND across the intestinal Caco-2 monolayer. The hydrophobic ion pairing of an OND and a cationic lipid served as an effective hydrophobization method using either dimethyldioctadecylammonium bromide (DDAB) or 1,2-dioleoyl-3-trimethylammonium propane (DOTAP). This strategy allowed a successful loading of OND-cationic lipid complexes into both negatively charged and neutral SEDDS. Subjecting both complex-loaded SEDDS to a nuclease, the negatively charged SEDDS protected about 16% of the complexed OND in contrast to 58% protected by its neutral counterpart. Furthermore, both SEDDS containing permeation-enhancing excipients facilitated delivery of OND across the intestinal Caco-2 cell monolayer. The negatively charged SEDDS showed a more stable permeability profile over 120 min, with a permeability of about 2 × 10−7 cm/s, unlike neutral SEDDS, which displayed an increasing permeability reaching up to 7 × 10−7 cm/s. In conclusion, these novel SEDDS-based formulations provide a promising tool for OND protection and delivery across the Caco-2 cell monolayer.

Nanoparticles with surface features of dendritic oligopeptides as potential oral drug delivery systems

2020 ◽  
Vol 8 (13) ◽  
pp. 2636-2649
Author(s):  
Yuli Bai ◽  
Rui Zhou ◽  
Lei Wu ◽  
Yaxian Zheng ◽  
Xi Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Specific Surface ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Protein Drugs ◽  
Surface Features ◽  
Oral Drug Delivery Systems

Endowing the NPs with specific surface features of dendritic oligopeptides holds great potential for the oral delivery of peptide/protein drugs.

Paliperidone-Loaded Self-Emulsifying Drug Delivery Systems (SEDDS) for Improved Oral Delivery

2012 ◽  
Vol 33 (4) ◽  
pp. 506-515 ◽  
Author(s):  
Swetha Kanuganti ◽  
Raju Jukanti ◽  
Prabhakar R. Veerareddy ◽  
Suresh Bandari
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems

scholarly journals Inflammatory Bowel Disease: The Emergence of New Trends in Lifestyle and Nanomedicine as the Modern Tool for Pharmacotherapy

Nanomaterials ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 2460
Author(s):  
Eden Mariam Jacob ◽  
Ankita Borah ◽  
Sindhu C Pillai ◽  
D. Sakthi Kumar
Keyword(s):  
Drug Delivery ◽  
Inflammatory Bowel Disease ◽  
Immune System ◽  
Bowel Disease ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Genetic Defect ◽  
Delivery Systems ◽  
Conventional Drug ◽  
Inflammatory Bowel

The human intestine, which harbors trillions of symbiotic microorganisms, may enter into dysbiosis when exposed to a genetic defect or environmental stress. The naissance of chronic inflammation due to the battle of the immune system with the trespassing gut bacteria leads to the rise of inflammatory bowel disease (IBD). Though the genes behind the scenes and their link to the disease are still unclear, the onset of IBD occurs in young adults and has expanded from the Western world into the newly industrialized countries. Conventional drug deliveries depend on a daily heavy dosage of immune suppressants or anti-inflammatory drugs targeted for the treatment of two types of IBD, ulcerative colitis (UC) and Crohn’s disease (CD), which are often associated with systemic side effects and adverse toxicities. Advances in oral delivery through nanotechnology seek remedies to overcome the drawbacks of these conventional drug delivery systems through improved drug encapsulation and targeted delivery. In this review, we discuss the association of genetic factors, the immune system, the gut microbiome, and environmental factors like diet in the pathogenesis of IBD. We also review the various physiological concerns required for oral delivery to the gastrointestinal tract (GIT) and new strategies in nanotechnology-derived, colon-targeting drug delivery systems.

scholarly journals Myristic Acid Coated Protein Immobilised Mesoporous Silica Particles as pH Induced Oral Delivery System for the Delivery of Biomolecules

2019 ◽  
Vol 12 (4) ◽  
pp. 153
Author(s):  
Vivek Trivedi ◽  
Ruchir Bhomia ◽  
John C Mitchell
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Protein Conformation ◽  
Myristic Acid ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Silica Particles ◽  
Protein Release ◽  
Simulated Gastric Fluid

Solid core drug delivery systems (SCDDS) were prepared for the oral delivery of biomolecules using mesoporous silica as core, bovine haemoglobin (bHb) as model drug and supercritical fluid (SCF) processing as encapsulation technique. The use of organic solvents or harsh processing conditions in the development of drug delivery systems for biomolecules can be detrimental for the structural integrity of the molecule. Hence, the coating on protein-immobilised particles was performed via supercritical carbon dioxide (scCO2) processing at a temperature lower than the melting point of myristic acid (MA) to avoid any thermal degradation of bHb. The SCDDS were prepared by bHb immobilisation on mesoporous silica followed by myristic acid (MA) coating at 43 °C and 100 bar in scCO2. bHb-immobilised silica particles were also coated via solvent evaporation (SE) to compare the protein release with scCO2 processed formulations. In both cases, MA coating provided required enteric protection and restricted the bHb release for the first two hours in simulated gastric fluid (SGF). The protein release was immediate upon the change of media to simulated intestinal fluid (SIF), reaching 70% within three hours. The release from SCF processed samples was slower than SE formulations, indicating superior surface coverage of MA on particles in comparison to the SE method. Most importantly, the protein conformation remained unchanged after the release from SCDDS as confirmed by circular dichroism. This study clearly demonstrates that the approach involving protein immobilisation on silica and scCO2 assisted melt-coating method can protect biomolecules from gastric environment and provide the required release of a biologic in intestine without any untoward effects on protein conformation during processing or after release.

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