Gastrointestinal contents in fasted state and post-lipid ingestion: In vivo measurements and in vitro models for studying oral drug delivery

Maio, Selena Di; Carrier, Rebecca L.

doi:10.1016/j.jconrel.2010.11.034

Cited by 79 publications

(67 citation statements)

References 113 publications

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“…In comparison, further CEF leakage of 11 % and 19 % from conventional liposomes was detected over 4 h in SGF and SGFpep, respectively. Facilitated permeation of CEF through the membrane was due to diffusion of protons from the media into the inner compartment compensation the ionic charge (45). Only minor change in vesicle size up to 4 h of incubation affirmed that the initial drug leakage is based on a proton gradient.…”

Section: Discussionmentioning

confidence: 92%

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Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

et al. 2017

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-PURPOSE: Liposomes have been studied as a colloidal carrier in drug delivery systems, especially for oral administration. However, their low structural integrity in the gut is still a major shortcoming. Membrane disruptive effects of physiological bile salts in the small intestine result in premature drug release prior to intestinal absorption. Thus, we analyzed the stabilizing effect of sodium deoxycholate when incorporated into nano-sized liposomes. METHOD: Cefotaxime-loaded liposomes were prepared with different sodium deoxycholate concentrations (3.75-30 mM) by rotary film evaporation followed by nanosize reduction. The physical integrity of liposomes was evaluated by monitoring cefotaxime leakage, particle sizes in different simulated physiological media. The oral bioavailability and pharmacokinetics of cefotaxime was assessed in rats (n = 6 per group) after single dose of drug-encapsulated in liposomes containing bile salt, drug in conventional liposomes, and cefotaxime solution (oral and intravenous). RESULTS: Simulated gastric fluid with low pH showed less effect on the stability of liposomes in comparison to media containing physiological bile salts. Liposomes containing 15 mM sodium deoxycholate were most stable in size and retained the majority of encapsulated cefotaxime even in fed state of simulated intestinal fluid being the most destructive media. Pharmacokinetics data showed an increase in Cmax and AUC0-inf in the following order: cefotaxime solution < conventional liposomes < liposomes made with bile salts. The total oral bioavailability of cefotaxime in liposomes containing bile salt was found to be 5-times higher compared to cefotaxime solution and twice as much as in conventional liposomes. CONCLUSION: Incorporation of bile salts, initially used as membrane permeation enhancer, also acted as a stabilizer against physiological bile salts. The nanosized liposomes containing sodium deoxycholate were able to reduce the leakage of encapsulated cefotaxime in the gut due to the improved vesicle stability and to enhance the oral bioavailability of acid-labile drugs up to 5-fold.

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Section: Discussionmentioning

confidence: 92%

“…It was shown that a 10 mM BS solution resulted in over 80% release of the entrapped marker from the vesicle. Physiological BS concentrations in the GIT range from 1 to 20 mM (45). Thus, we tested the stability of our nano-vesicles formulations in FaSSIF and FeSSIF solution containing NaTC in a concentration of 3.75 and 15 mM, respectively.…”

Section: Discussionmentioning

confidence: 99%

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

et al. 2017

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“…The difference between the s and p spectra provides information on species present at the interface while the sum is the reference spectrum. Experiments were performed in DDG monolayers in the presence and absence of chitosan with the surface pressure at 30 mN m −1 , which is the value corresponding to cell membranes in in vivo experiments [55]. When the surface pressure reached 30 mN m −1 , 5.0 mL of a 0.070 g L −1 HPL stock solution was injected behind the barrier.…”

Section: Methodsmentioning

confidence: 99%

Chitosan does not inhibit enzymatic action of human pancreatic lipase in Langmuir monolayers of 1,2-didecanoyl-glycerol (DDG)

Souza

Pavinatto

Caseli

et al. 2014

Colloids and Surfaces B: Biointerfaces

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“…During the last decades, the thorough physicochemical characterisation of human gastrointestinal fluids allowed the development of biorelevant media closer matching the in vivo conditions compared with the rather simple compendial media (43)(44)(45). The proposed biorelevant media contain physiological relevant amounts of buffer, lecithin and bile salts mimicking either the fasted or fed state (Table I) and have been subject of recent reviews (46,47).…”

Section: Dispersion Testing Of Lbddsmentioning

confidence: 99%

Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development

Thomas

Holm

Rades

2012

AAPS J

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Abstract. Facing the increasing number of poorly water-soluble drugs, pharmaceutical scientists are required to break new grounds for the delivery of these pharmaceutically problematic drugs. Lipid-based drug delivery systems (LBDDS) have received increased interest as a novel drug delivery platform during the last decades and several successfully marketed products have shown the potential for LBDDS. However, there exists a discrepancy between the clear need for innovative delivery forms and their rational design. In the case of LBDDS, this can be attributed to the complexity of LBDDS after administration. Unlike conventional formulations, LBDDS are susceptible to digestion in the gastrointestinal tract, the interplay of delivery system, drug and physiology ultimately effecting drug disposition. In vitro lipolysis has become an important technique to mimic the enzymatic degradation. For the better understanding of how LBDDS promote drug delivery, in vitro lipolysis requires advanced characterisation methods. In this review, the physiological background of lipid digestion is followed by a thorough summary of the techniques that are currently used to characterise in vitro lipolysis. It would be desirable that the increasing knowledge about LBDDS will foster their rationale development thereby increasing their broader application.KEY WORDS: in vitro digestion; in vitro lipolysis models; lipid-based drug delivery systems; poorly soluble drugs; self-nanoemulsifying drug delivery systems (SNEDDS).

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Gastrointestinal contents in fasted state and post-lipid ingestion: In vivo measurements and in vitro models for studying oral drug delivery

Cited by 79 publications

References 113 publications

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

Nanosized Liposomes Containing Bile Salt: A Vesicular Nanocarrier for Enhancing Oral Bioavailability of BCS Class III Drug

Chitosan does not inhibit enzymatic action of human pancreatic lipase in Langmuir monolayers of 1,2-didecanoyl-glycerol (DDG)

Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development

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