scholarly journals Transfer of Lipophilic Drugs from Nanoemulsions into Lipid-Containing Alginate Microspheres

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 173
Author(s):  
Sabrina Knoke ◽  
Heike Bunjes
Keyword(s):  
Interfacial Area ◽  
Water Soluble ◽  
Good Time ◽  
Retinyl Acetate ◽  
Hydrogel Beads ◽  
Physiological Conditions ◽  
System A ◽  
Water Soluble Drugs ◽  
Filtration Step

Knowledge about the release behavior and drug retention properties of colloidal carriers is of essential importance for quality control as well as to predict in vivo performance. When conducting release studies from such systems, the release media should preferentially contain lipophilic acceptor components in order to mimic physiological conditions. In this study, transfer from a trimyristin nanoemulsion into lipid-containing hydrogel beads was investigated for fenofibrate, cannabidiol, retinyl acetate, orlistat, and lumefantrine. To generate the acceptor system, a trimyristin nanoemulsion was incorporated into Ca-alginate microspheres (mean diameter ~40 µm) with a spraying method. Using this approach, the advantages of small lipophilic acceptor particles with a large interfacial area were combined with a single separation process from the donor via a filtration step. The method was applicable to distinguish between fast (fenofibrate) and slow drug transfer (lumefantrine) with good time resolution. Lipophilicity, estimated according to the calculated logP value of the respective drug, was a major factor influencing the transfer performance: the higher the logP value, the slower the transfer. This experimental setup is a promising technique to investigate the release of poorly water-soluble drugs from various types of nanocarriers under closer to physiological conditions than with many other methods currently applied.

scholarly journals Transfer Investigations of Lipophilic Drugs from Lipid Nanoemulsions to Lipophilic Acceptors: Contributing Effects of Cholesteryl Esters and Albumin as Acceptor Structures

2021 ◽  
Vol 14 (9) ◽  
pp. 865
Author(s):  
Sabrina Knoke ◽  
Heike Bunjes
Keyword(s):  
Liquid Solution ◽  
Water Soluble ◽  
Retinyl Acetate ◽  
Lipophilic Drugs ◽  
Emulsion Droplets ◽  
Hydrogel Particles ◽  
Water Soluble Drugs ◽  
Partition Equilibrium ◽  
Poorly Water Soluble

When studying the release of poorly water-soluble drugs from colloidal drug delivery systems designed for intravenous administration, the release media should preferentially contain lipophilic components that represent the physiological acceptors present in vivo. In this study, the effect of different acceptor structures was investigated by comparing the transfer of fenofibrate, retinyl acetate, and orlistat from trimyristin nanoemulsion droplets into lipid-containing hydrogel particles, as well as to bovine serum albumin (BSA). A nanodispersion based on trimyristin and cholesteryl nonanoate was incorporated into the hydrogel particles (mean diameter ~40 µm) in order to mimic the composition of lipoproteins. The course of transfer observed utilizing the lipid-containing hydrogel particles as an acceptor was in relation to the lipophilicity of the drugs: the higher the logP value, the slower the transfer. There was no detectable amount of the drugs transferred to BSA in liquid solution, demonstrating clearly that albumin alone does not contribute substantially as acceptor for the lipophilic drugs under investigation in this study. In contrast, cholesteryl nonanoate contributes to a much greater extent. However, in all cases, the partition equilibrium of the drugs under investigation was in favor of the trimyristin emulsion droplets.

scholarly journals Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

2011 ◽  
Vol 47 (3) ◽  
pp. 447-465 ◽  
Author(s):  
Jyoti Wadhwa ◽  
Anroop Nair ◽  
Rachna Kumria
Keyword(s):  
Drug Disposition ◽  
Water Soluble ◽  
Therapeutic System ◽  
System A ◽  
Gastrointestinal Fluid ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
The Impact

Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.

scholarly journals Sterically Stabilized RIPL Peptide-Conjugated Nanostructured Lipid Carriers: Characterization, Cellular Uptake, Cytotoxicity, and Biodistribution

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 199 ◽  
Author(s):  
Chang Kim ◽  
Si Sung ◽  
Eun Lee ◽  
Tae Kang ◽  
Ho Yoon ◽  
...  
Keyword(s):  
Drug Loading ◽  
Mononuclear Phagocyte ◽  
Nanostructured Lipid Carriers ◽  
Water Soluble ◽  
Zeta Potentials ◽  
Grafting Ratio ◽  
Macrophage Phagocytosis ◽  
Water Soluble Drugs ◽  
High Payload

As a platform for hepsin-specific drug delivery, we previously prepared IPLVVPLRRRRRRRRC peptide (RIPL)-conjugated nanostructured lipid carriers (RIPL-NLCs) composed of Labrafil® M 1944 CS (liquid oil) and Precirol® ATO 5 (solid lipid). In this study, to prevent the recognition by the mononuclear phagocyte system, polyethylene glycol (PEG)-modified RIPL-NLCs (PEG-RIPL-NLCs) were prepared using PEG3000 at different grafting ratios (1, 5, and 10 mole %). All prepared NLCs showed a homogeneous dispersion (130–280 nm), with zeta potentials varying from −18 to 10 mV. Docetaxel (DTX) was successfully encapsulated in NLCs: encapsulation efficiency (93–95%); drug-loading capacity (102–109 µg/mg). PEG-RIPL-NLCs with a grafting ratio of 5% PEG or higher showed significantly reduced protein adsorption and macrophage phagocytosis. The uptake of PEG(5%)-RIPL-NLCs by cancer cell lines was somewhat lower than that of RIPL-NLCs because of the PEG-induced steric hindrance; however, the uptake level of PEG-RIPL-NLCs was still greater than that of plain NLCs. In vivo biodistribution was evaluated after tail vein injection of NLCs to normal mice. Compared to RIPL-NLCs, PEG(5%)-RIPL-NLCs showed lower accumulation in the liver, spleen, and lung. In conclusion, we found that PEG(5%)-RIPL-NLCs could be a promising nanocarrier for selective drug targeting with a high payload of poorly water-soluble drugs.

Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets

2019 ◽  
Vol 4 (2) ◽  
pp. 121-129
Author(s):  
Satya Sankar Sahoo ◽  
Chandu Babu Rao
Keyword(s):  
Patient Compliance ◽  
Oral Drug Delivery ◽  
Particle Diameter ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Water Soluble Drugs ◽  
Fast Disintegrating Tablets ◽  
Lurasidone Hydrochloride

Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.

scholarly journals Ternary Solid Dispersion Strategy for Solubility Enhancement of Poorly Soluble Drugs by Co-Milling Technique

2021 ◽  
Author(s):  
Marouene Bejaoui ◽  
Hanen Oueslati ◽  
Haykel Galai
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
Water Soluble ◽  
Pharmaceutical Ingredients ◽  
Drug Molecules ◽  
Water Soluble Drugs ◽  
Milling Method ◽  
Ternary Solid Dispersion

Amorphous ternary solid dispersion has become one of the strategies commonly used for improving the solubility and bioavailability of poorly water soluble drugs. Such multicomponent solid dispersion can be obtained by different techniques, this chapter provides an overview of ternary solid dispersion by co-milling method from the perspectives of physico-chemical characteristics in vitro and in vivo performance. A considerable improvement of solubility was obtained for many active pharmaceutical ingredients (e.g., Ibuprofen, Probucol, Gliclazid, Fenofibrate, Ibrutinib and Naproxen) and this was correlated to the synergy of multiple factors (hydrophilicity enhancement, particle size reduction, drug-carrier interactions, anti-plasticizing effect and complexation efficiency). This enhanced pharmacokinetic properties and bioavailability of these drug molecules (1.49 to 15-folds increase in plasma drug concentration). A particular focus was accorded to compare the ternary and binary system including Ibuprofen and highlighting the contribution of thermal and spectral characterization techniques. The addition of polyvinylpyrrolidone (PVP K30), a low molecular weight molecule, into the binary solid dispersion (Ibuprofen/β-cyclodextrin), leads to a 1.5–2 folds increase in the drug intrinsic dissolution rate only after 10 min. This resulted from physical stabilization of amorphous Ibuprofen by reducing its molecular mobility and inhibiting its recristallization even under stress conditions (75% RH and T = 40°C for six months).

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