Mechanism and kinetics of the loss of poorly soluble drugs from liposomal carriers studied by a novel flow field-flow fractionation-based drug release −/transfer-assay

Hinna, Askell; Hupfeld, Stefan; Kuntsche, Judith; Bauer‐Brandl, Annette; Brandl, Martin

doi:10.1016/j.jconrel.2016.04.031

Cited by 29 publications

(19 citation statements)

References 36 publications

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“…Nevertheless, sampling the release medium requires a suitable separation method, which poses the same disadvantages cited before [157]. A series of articles [129,[158][159][160] demonstrated how AF4 can perform drug release and drug transfer studies [195] Other proteins/peptides Esterase (porcine liver), myoglobin (equine skeletal muscle)…”

Section: Release Of Lipophilic Drugsmentioning

confidence: 99%

Asymmetric flow field-flow fractionation as a multifunctional technique for the characterization of polymeric nanocarriers

Quattrini

Berrecoso

Crecente‐Campo

et al. 2021

Drug Deliv. and Transl. Res.

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The importance of polymeric nanocarriers in the field of drug delivery is ever-increasing, and the accurate characterization of their properties is paramount to understand and predict their behavior. Asymmetric flow field-flow fractionation (AF4) is a fractionation technique that has gained considerable attention for its gentle separation conditions, broad working range, and versatility. AF4 can be hyphenated to a plurality of concentration and size detectors, thus permitting the analysis of the multifunctionality of nanomaterials. Despite this potential, the practical information that can be retrieved by AF4 and its possible applications are still rather unfamiliar to the pharmaceutical scientist. This review was conceived as a primer that clearly states the “do’s and don’ts” about AF4 applied to the characterization of polymeric nanocarriers. Aside from size characterization, AF4 can be beneficial during formulation optimization, for drug loading and drug release determination and for the study of interactions among biomaterials. It will focus mainly on the advances made in the last 5 years, as well as indicating the problematics on the consensus, which have not been reached yet. Methodological recommendations for several case studies will be also included. Graphical abstract

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Section: Release Of Lipophilic Drugsmentioning

confidence: 99%

Asymmetric flow field-flow fractionation as a multifunctional technique for the characterization of polymeric nanocarriers

Quattrini

Berrecoso

Crecente‐Campo

et al. 2021

Drug Deliv. and Transl. Res.

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“…Here, we prepared a liposome formulation for curcumin application in vivo based on the excellent drug-loading performance of the liposomal carrier that not only improves the water solubility of poorly soluble drugs but also facilitates drug targeting and controlled release after modification. 29,30 The aqueous solution of the prepared liposomes appeared yellow under visible light (Figure 2A-a) and exhibited green florescence under UV light (Figure 2A-b). When fluorescence of the liposome solution was excited at 440 nm, its emission wavelength located at 475 nm, which was consistent with that of free curcumin ( Figure 2B).…”

Section: Results and Discussion Characteristics Of The Nanoliposomesmentioning

confidence: 99%

Targeted therapy of intracranial glioma model mice with curcumin nanoliposomes

Zhao¹,

Zhao²,

Fu³

et al. 2018

IJN

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BackgroundGlioma is the most aggressive and lethal brain tumor in humans, it comprises about 30 per cent of all brain tumors and central nervous system tumors.PurposeThe objective of this study was to create novel brain-targeting nanoliposomes to encapsulate curcumin as a promising option for glioma therapy.Patients and methodsHuman glioma cells (U251MG) were used to determine cell uptake efficiency and possible internalization mechanism of the curcumin-loaded nanoliposomes modified by a brain-targeting peptide RDP. In addition, intracranial glioma mice model was prepared by transplantation of U251MG cells into the mice striatum, and then the liposomes were intravenously administered into the glioma-bearing mice to evaluate the anti-glioma activity.ResultsRDP-modified liposomes (RCL) could enter the brain and glioma region, and were internalized by the glioma cells perhaps through acetylcholine receptor-mediated endocytosis pathway. Furthermore, the RCL prolonged the survival time of the glioma-bearing mice from 23 to 33 days, and the inhibition mechanism of the RCL on glioma cell was partly due to cell cycle arrest at the S phase and induction of cell apoptosis.ConclusionThis study would provide a potential approach for targeted delivery of drug-loaded liposomes for glioma treatment.

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“…Lipophilic prodrugs and liposomes are promising strategies for prolonging the effect time in vivo and improving the other shortcomings of CA4. The use of lipophilic prodrugs can improve the absorption, distribution, metabolism, and excretion profiles for parenteral administration; lipophilic therapeutics also exhibit greater half-lives 9,24. Liposomes are nano-agents composed of phospholipids with excellent biodegradability, biocompatibility, and low toxicity; they are an ideal carrier system for drug delivery 25.…”

Section: Introductionmentioning

confidence: 99%

<p>Development Of Novel Liposome-Encapsulated Combretastatin A4 Acylated Derivatives: Prodrug Approach For Improving Antitumor Efficacy</p>

Gu¹,

Ma²,

Fu³

et al. 2019

IJN

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PurposeThe objective of the present study was to develop a liposomal drug delivery system based on combretastatin A4 (CA4) prodrugs modified with varying alkyl chains and investigate the in vitro drug conversion from prodrug and in vivo antitumor effect.MethodsThe prodrug of CA4 was synthesized with stearyl chloride (18-carbon chain), palmitoyl chloride (16-carbon chain), myristoyl chloride (14-carbon chain), decanoyl chloride (10-carbon chain), and hexanoyl chloride (6-carbon chain) at the 3′-position of the CA4. Subsequently, it was encapsulated with liposomes through the thin-film evaporation method. Furthermore, the characteristics of prodrug-liposome were evaluated using in vitro drug release, conversion, and cytotoxicity assays, as well as in vivo pharmacokinetic, antitumor, and biodistribution studies.ResultsThe liposome system with loaded CA4 derivatives was successfully developed with nano-size and electronegative particles. The rate of in vitro drug release and conversion was reduced as the fatty acid carbon chain lengthened. On the contrary, in vivo antitumor effects were improved with the enlargement of the fatty acid carbon chain. The results of the in vivo pharmacokinetic and tissue distribution studies indicated that the reduced rate of CA4 release with a long carbon chain could prolong the circulation time and increase the drug concentration in the tumor tissue.ConclusionThese results suggested that the release or hydrolysis of the parent drug from the prodrug was closely related with the in vitro and in vivo properties. The slow drug release of CA4 modified with longer acyl chain could prolong the circulation time and increase the concentration of the drug in the tumor tissue. These effects play a critical role in increasing the antitumor efficacy.

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Mechanism and kinetics of the loss of poorly soluble drugs from liposomal carriers studied by a novel flow field-flow fractionation-based drug release −/transfer-assay

Cited by 29 publications

References 36 publications

Asymmetric flow field-flow fractionation as a multifunctional technique for the characterization of polymeric nanocarriers

Asymmetric flow field-flow fractionation as a multifunctional technique for the characterization of polymeric nanocarriers

Targeted therapy of intracranial glioma model mice with curcumin nanoliposomes

<p>Development Of Novel Liposome-Encapsulated Combretastatin A4 Acylated Derivatives: Prodrug Approach For Improving Antitumor Efficacy</p>

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