Surface design of nanocarriers: Key to more efficient oral drug delivery systems

Spleis, Helen; Sandmeier, Matthias; Claus, Victor; Bernkop‐Schnürch, Andreas

doi:10.1016/j.cis.2023.102848

Cited by 28 publications

(16 citation statements)

References 212 publications

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“…NS@lipid-PEG/CKC (0.02%) with higher positive zeta potential showed higher cellular uptake by HCECs at 4 and 6 h (Figure A). According to the literature, the positively charged nanomedicine may be electrostatically attracted by the negatively charged cell membrane, leading to increased membrane fluidity and membrane wrapping. , Furthermore, the cellular uptake of the positively charged nanomedicine is predominantly through micropinocytosis, which might also be true for NS@lipid-PEG/CKC reported here, whereas the negatively charged nanomedicine is suggested to be taken up via clathrin-/caveolae-independent endocytosis. , The specific cellular uptake mechanism of NS@lipid-PEG/CKC will be explored in future research.…”

Section: Resultsmentioning

confidence: 72%

Combination of PEGylation and Cationization on Phospholipid-Coated Cyclosporine Nanosuspensions for Enhanced Ocular Drug Delivery

Ma,

Liu,

Wang

et al. 2024

ACS Appl. Mater. Interfaces

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Strong precorneal clearance mechanisms including reflex blink, constant tear drainage, and rapid mucus turnover constitute great challenges for eye drops for effective drug delivery to the ocular epithelium. In this study, cyclosporine A (CsA) for the treatment of dry eye disease (DED) was selected as the model drug. Two strategies, PEGylation for mucus penetration and cationization for potent cellular uptake, were combined to construct a novel CsA nanosuspension (NS@lipid-PEG/CKC) by coating nanoscale drug particles with a mixture of lipids, DSPE-PEG2000, and a cationic surfactant, cetalkonium chloride (CKC). NS@lipid-PEG/CKC with the mean size ∼173 nm and positive zeta potential ∼+40 mV showed promoted mucus penetration, good cytocompatibility, more cellular uptake, and prolonged precorneal retention without obvious ocular irritation. More importantly, NS@lipid-PEG/CKC recovered tear production and goblet cell density more efficiently than the commercial cationic nanoemulsion on a dry eye disease rat model. All results indicated that a combination of PEGylation and cationization might provide a promising strategy to coordinate mucus penetration and cellular uptake for enhanced drug delivery to the ocular epithelium for nanomedicine-based eye drops.

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Section: Resultsmentioning

confidence: 72%

Combination of PEGylation and Cationization on Phospholipid-Coated Cyclosporine Nanosuspensions for Enhanced Ocular Drug Delivery

Ma,

Liu,

Wang

et al. 2024

ACS Appl. Mater. Interfaces

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“…So far, numerous nanoparticle‐based systems such as polymeric nanoparticles, lipid‐based nanoparticles (LNPs) and extracellular vesicles (EVs) have been developed for oral nucleic acid delivery. Nucleic acids are encapsulated and protected in nanoparticles, which frees them from degradation in physiological environments 8,11 …”

Section: Introductionmentioning

confidence: 99%

“…Nucleic acids are encapsulated and protected in nanoparticles, which frees them from degradation in physiological environments. 8,11 The increasing global attention on nucleic acid delivery systems has led to innovations in overcoming various biological barriers. 12 Current nucleic acid therapeutic delivery systems can be broadly divided into virus-based carriers and non-viral carriers.…”

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confidence: 99%

Nanoparticles derived from herbal preparations May represent a novel nucleic acid therapy

Feng,

Ahmed,

Ahmed

et al. 2024

Interdisciplinary Medicine

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A significant number of nucleic acid therapies have been approved, highlighting the vast potential of nucleic acid therapeutics. Although numerous delivery strategies have been investigated, and progress has been made in nucleic acid delivery systems, the oral delivery route still presents a significant obstacle. Recently, a novel and promising force in oral nucleic acid delivery has emerged, namely Decoctosomes and Bencaosomes, obtained from the decoction of natural herbs, which refers to boiled Chinese herbal medicines. The active components of Decoctosomes include small molecules, peptides, and small RNAs (sRNAs). sRNAs were the first targets of extensive research. Additionally, Bencaosomes have been proven effective in several disease mouse models as artificially enhanced decoctosome products. This perspective summarizes the development and possible future directions of Decoctosomes and Bencaosomes, two varieties of nanoparticles that may open the door to new possibilities in nucleic acid therapy.

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“…This technique involves the attachment of polymers and ligands to the outer layer of nanoparticles, which reduces their interaction with mucus components and facilitates their movement within the mucus environment. 15 Various methods have been explored to improve nanoparticle penetration through the intestinal mucus layer. These methods include surface modification through PEGylation, the attachment of mucuspenetrating peptides, conjugation with ligands that bind to specific receptors on the mucosal surface, and optimization of size and surface charge.…”

Section: Introductionmentioning

confidence: 99%

“…Surface modification of nanoparticles represents a promising approach for enhancing their ability to penetrate mucus. This technique involves the attachment of polymers and ligands to the outer layer of nanoparticles, which reduces their interaction with mucus components and facilitates their movement within the mucus environment . Various methods have been explored to improve nanoparticle penetration through the intestinal mucus layer.…”

Section: Introductionmentioning

confidence: 99%

Bromelain-Decorated Nanoscale Liposomes for Mucus Permeation and Intestinal Absorption in Oral Drug Delivery

Park,

Choi,

Kang

et al. 2023

ACS Appl. Nano Mater.

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Nanoscale liposomes are widely recognized as promising drug delivery materials; yet, their utilization in oral drug delivery has been hindered by their limited ability to efficiently penetrate the intestinal mucus layer. Herein, we present an approach to enhance oral drug delivery and improve the mucus penetration capability of liposomes by conjugating bromelain, a mucolytic enzyme derived from pineapple stems, to the liposome membrane (Bro-Lip). With an optimized bromelain payload of 11.1 nmol/mg, we achieved an impressive 47.8% conjugation efficiency while retaining 77.5% of the proteolytic activity post conjugation. Physicochemical analysis revealed that Bro-Lip measured 152.8 nm in size with a ζ potential of −2.3 mV. Notably, Bro-Lip exhibited a significantly enhanced capacity to penetrate the porcine mucus layer, demonstrating a 2.87-fold improvement compared with bare liposomes. Furthermore, we assessed the transcellular permeability of Bro-Lips using Caco-2 and Caco-2/HT29 coculture models, revealing substantial enhancements in permeability compared to unmodified liposomes. Specifically, in Caco-2 cell monolayers, mucus permeability increased by 3.80-fold, while in Caco-2/HT29 cocultures, it rose by 2.25-fold. Additionally, Bro-Lip demonstrated an improved cellular uptake in Caco-2 cells. These findings highlight the potential of Bro-Lip as an effective oral delivery system by enhancing mucus permeation and cell membrane permeation.

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Surface design of nanocarriers: Key to more efficient oral drug delivery systems

Cited by 28 publications

References 212 publications

Combination of PEGylation and Cationization on Phospholipid-Coated Cyclosporine Nanosuspensions for Enhanced Ocular Drug Delivery

Combination of PEGylation and Cationization on Phospholipid-Coated Cyclosporine Nanosuspensions for Enhanced Ocular Drug Delivery

Nanoparticles derived from herbal preparations May represent a novel nucleic acid therapy

Bromelain-Decorated Nanoscale Liposomes for Mucus Permeation and Intestinal Absorption in Oral Drug Delivery

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