Three-dimensional liposome networks: freeze fracture electron microscopical evaluation of their structure and in vitro analysis of release of hydrophilic markers

Brandl, Martin; Tardi, Christine; Drechsler, Markus; Bachmann, Dieter; Reszka, Regina; Bauer, Karl-Heinrich; Schubert, Rolf

doi:10.1016/s0169-409x(96)00455-3

Cited by 17 publications

(5 citation statements)

References 5 publications

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“…29 In addition, use of formulations with high EE has the benefit that there is no need to remove the unencapsulated drug before use, making the production process more efficient. [30][31][32] In order to investigate the effect of SPC content on the EE of VPG liposomes for SBS, a series of liposome dispersions were prepared with increasing SPC/VPG from 250 to 500 mg/g. The EE was determined as the ratio of SBS concentration in the vesicle core to that in the total liposome suspension.…”

Section: Results and Discussion Preparation Of Sbs Vpg And Sbs Dir Vpgmentioning

confidence: 99%

Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery

Chen¹,

Huang²,

Wong³

et al. 2012

IJN

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Purpose:The main objective of this study was to develop a novel aerosolized liposome formulation for pulmonary delivery of anti-asthmatic medication and to explore the relationship between the bioavailability and anti-asthmatic efficacy of such a formulation. Asthma treatment usually requires frequent administration of medication for sustained bronchodilating response. Liposomes are known for their capability for sustained drug release and thus would be a suitable delivery system for anti-asthmatic medication for prolonged therapeutic effect. Salbutamol sulfate (SBS) was chosen as the model drug in this study because of its high water solubility and fast absorption after administration. Methods: SBS was efficiently encapsulated into liposomes by the vesicular phospholipid gel technique. SBS permeability across the pulmonary membrane of an Asian toad was determined by in vitro study. Intratracheal administration of liposomes labeled with the fluorescent dye 1,1′-dioctadecyltetramethyl indotricarbocyanine iodide (DiR) in a rat model was assessed by a small animal imaging system and pharmacokinetic analysis. Pharmacodynamic analysis was performed in guinea pigs using the Konzett-Rössler method. Results: SBS was efficiently encapsulated into liposomes with encapsulation efficiency as high as 70%. The particle size of the SBS liposome suspension was approximately 57 ± 21 nm. In the in vitro study of permeability across the pulmonary membrane of Asian toads, SBS from liposomes demonstrated a slower transport rate compared to free SBS solution. Pulmonary delivery of liposomes in a rat model showed that the liposomes were effectively distributed in the respiratory tract and lungs, and that the release of SBS from liposomes was sustained for at least 48 hours. Pharmacodynamic analysis in a guinea pig model showed that the anti-asthmatic effect of SBS liposomes persisted for up to 18 hours, whereas that of free SBS solution was less than 8 hours. Conclusion:The overall results demonstrated that liposomes could increase the concentration and retention time of SBS in the lungs and therefore prolong its therapeutic effect.

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Section: Results and Discussion Preparation Of Sbs Vpg And Sbs Dir Vpgmentioning

confidence: 99%

Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery

Chen¹,

Huang²,

Wong³

et al. 2012

IJN

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“…To clinically evaluate efficacy of BSASM preparation, three kinds of formulations containing BSASM preparation were prepared; face/body wash, liposome lotion, and liposome serum which contain 1, 1.5, and 3% of BSASM preparation, respectively. Liposome lotion and liposome serum were manufactured in a base of liposome by using the one-step homogenization technique as described in Brandl et al (1997). Face/body wash is a general liquid soap with a low level of detergent.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of the anti-inflammatory and atopic dermatitis-mitigating effects of BSASM, a multicompound preparation

Lee¹,

Jung²,

Park³

et al. 2005

Journal of Ethnopharmacology

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“…In contrast to its predecessor, the PermeaPad does not contain preformed liposomes. Instead, in the PermeaPad barrier, a liposomal gel [ 76 ] forms upon contact with water ( Figure 10 ). Specifically, the thin, dry phospholipid layer hydrates and swells between the two regenerated cellulose layers (with an estimated cut-off size of 7–10 kDa).…”

Section: Commercially Available Biomimetic Cell-free In Vitro Permeab...mentioning

confidence: 99%

“…In another part of this study, Jacobsen et al investigated the structure of the PermeaPad barrier via light microscopy [ 77 ]. This resulted in the first pictures of the peculiar liposomal structures that formed between the two cellulose sheets upon hydration, i.e., a constrained vesicular phospholipid gel [ 76 ].…”

Section: Commercially Available Biomimetic Cell-free In Vitro Permeab...mentioning

confidence: 99%

Commercially Available Cell-Free Permeability Tests for Industrial Drug Development: Increased Sustainability through Reduction of In Vivo Studies

et al. 2023

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Replacing in vivo with in vitro studies can increase sustainability in the development of medicines. This principle has already been applied in the biowaiver approach based on the biopharmaceutical classification system, BCS. A biowaiver is a regulatory process in which a drug is approved based on evidence of in vitro equivalence, i.e., a dissolution test, rather than on in vivo bioequivalence. Currently biowaivers can only be granted for highly water-soluble drugs, i.e., BCS class I/III drugs. When evaluating poorly soluble drugs, i.e., BCS class II/IV drugs, in vitro dissolution testing has proved to be inadequate for predicting in vivo drug performance due to the lack of permeability interpretation. The aim of this review was to provide solid proofs that at least two commercially available cell-free in vitro assays, namely, the parallel artificial membrane permeability assay, PAMPA, and the PermeaPad® assay, PermeaPad, in different formats and set-ups, have the potential to reduce and replace in vivo testing to some extent, thus increasing sustainability in drug development. Based on the literature review presented here, we suggest that these assays should be implemented as alternatives to (1) more energy-intense in vitro methods, e.g., refining/replacing cell-based permeability assays, and (2) in vivo studies, e.g., reducing the number of pharmacokinetic studies conducted on animals and humans. For this to happen, a new and modern legislative framework for drug approval is required.

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Three-dimensional liposome networks: freeze fracture electron microscopical evaluation of their structure and in vitro analysis of release of hydrophilic markers

Cited by 17 publications

References 5 publications

Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery

Liposomes prolong the therapeutic effect of anti-asthmatic medication via pulmonary delivery

Evaluation of the anti-inflammatory and atopic dermatitis-mitigating effects of BSASM, a multicompound preparation

Commercially Available Cell-Free Permeability Tests for Industrial Drug Development: Increased Sustainability through Reduction of In Vivo Studies

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