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Tomizawa, Hitoshi; Aramaki, Yukihiko; Fujii, Yoshimine; Hara, Toshifumi; Suzuki, Norihiro; Yachi, Kiyoto; Kikuchi, Hiroshi; Tsuchiya, Satoshi

doi:10.1023/a:1018945902276

Cited by 47 publications

(14 citation statements)

References 15 publications

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“…, 186. , and the liposomal surface charges influenced the efficency 187 . In addition, prolonged residence of liposomes in GIT increases the opportunity of uptake by M cells 188.…”

Section: Mechanisms Of Oral Absorption Of Liposomesmentioning

confidence: 99%

“…Therefore, M cells are easily accessible for liposomes via mechanisms of adsorptive endocytosis, fluid phase endocytosis and phagocytosis 185 . It was shown that the M cell pathway contributes to total oral absorption of liposomes57., 186., and the liposomal surface charges influenced the efficency 187 . In addition, prolonged residence of liposomes in GIT increases the opportunity of uptake by M cells188., 189., which partly explains the contribution of stabilization of liposomes to enhanced oral absorption69., 95..…”

Section: Mechanisms Of Oral Absorption Of Liposomesmentioning

confidence: 99%

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Adapting liposomes for oral drug delivery

Lü

et al. 2019

Acta Pharmaceutica Sinica B

476

250

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Liposomes mimic natural cell membranes and have long been investigated as drug carriers due to excellent entrapment capacity, biocompatibility and safety. Despite the success of parenteral liposomes, oral delivery of liposomes is impeded by various barriers such as instability in the gastrointestinal tract, difficulties in crossing biomembranes, and mass production problems. By modulating the compositions of the lipid bilayers and adding polymers or ligands, both the stability and permeability of liposomes can be greatly improved for oral drug delivery. This review provides an overview of the challenges and current approaches toward the oral delivery of liposomes.

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“…, 186. , and the liposomal surface charges influenced the efficency 187 . In addition, prolonged residence of liposomes in GIT increases the opportunity of uptake by M cells 188.…”

Section: Mechanisms Of Oral Absorption Of Liposomesmentioning

confidence: 99%

Section: Mechanisms Of Oral Absorption Of Liposomesmentioning

confidence: 99%

Adapting liposomes for oral drug delivery

Lü

et al. 2019

Acta Pharmaceutica Sinica B

476

250

View full text Add to dashboard Cite

show abstract

“…The uptake of particles is reported to primarily occur via the M cells [2], which have been referred to provide a privileged contact with mannose residues [14,15] and, therefore, might be used as privileged target for mannose-containing particles. Locust bean gum (LBG) is a polysaccharide of the class of galactomannans, thus having a chemical structure composed of both galactose and mannose units [16] (Fig.…”

Section: Introductionmentioning

confidence: 99%

Chitosan/sulfated locust bean gum nanoparticles: In vitro and in vivo evaluation towards an application in oral immunization

Braz

Grenha

Ferreira

et al. 2017

International Journal of Biological Macromolecules

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This work proposes the design of nanoparticles based on locus bean gum (LBG) and chitosan to be used as oral immunoadjuvant for vaccination purposes. LBG-based nanoparticles were prepared by mild polyelectrolyte complexation between chitosan (CS) and a synthesized LBG sulfate derivative (LBGS). Morphological characterization suggested that nanoparticles present a solid and compact structure with spherical-like shape. Sizes around 180-200nm and a positive surface charge between +9mV and +14mV were obtained. CS/LBGS nanoparticles did not affect cell viability of Caco-2 cells after 3h and 24h of exposure when tested at concentrations up to 1.0mg/mL. Two model antigens (a particulate acellular extract HE of Salmonella enterica serovar Enteritidis, and ovalbumin as soluble antigen) were associated to CS/LBGS nanoparticles with efficiencies around 26% for ovalbumin and 32% for HE, which resulted in loading capacities up to 12%. The process did not affect the antigenicity of the associated antigens. BALB/c mice were orally immunized with ovalbumin-loaded nanoparticles (100μg), and results indicate an adjuvant effect of the CS/LBGS nanoparticles, eliciting a balanced Th1/Th2 immune response. Thus, CS/LBGS nanoparticles are promising as antigen mucosal delivery strategy, with particular interest for oral administration.

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“…There are several reports on the intact liposomal uptake by cells in in vitro and in situ experiments56–58. The results are, however, not convincing for the oral delivery of protein with a liposomal system.…”

Section: Pharmaceutical Approachesmentioning

confidence: 98%

Protein and peptide drug delivery: Oral approaches

Shaji¹,

Patole²

2008

Indian J Pharm Sci

227

118

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Till recent, injections remained the most common means for administering therapeutic proteins and peptides because of their poor oral bioavailability. However, oral route would be preferred to any other route because of its high levels of patient acceptance and long term compliance, which increases the therapeutic value of the drug. Designing and formulating a polypeptide drug delivery through the gastro intestinal tract has been a persistent challenge because of their unfavorable physicochemical properties, which includes enzymatic degradation, poor membrane permeability and large molecular size. The main challenge is to improve the oral bioavailability from less than 1% to at least 30-50%. Consequently, efforts have intensified over the past few decades, where every oral dosage form used for the conventional small molecule drugs has been used to explore oral protein and peptide delivery. Various strategies currently under investigation include chemical modification, formulation vehicles and use of enzyme inhibitors, absorption enhancers and mucoadhesive polymers. This review summarizes different pharmaceutical approaches which overcome various physiological barriers that help to improve oral bioavailability that ultimately achieve formulation goals for oral delivery.

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Cited by 47 publications

References 15 publications

Adapting liposomes for oral drug delivery

Adapting liposomes for oral drug delivery

Chitosan/sulfated locust bean gum nanoparticles: In vitro and in vivo evaluation towards an application in oral immunization

Protein and peptide drug delivery: Oral approaches

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