The interaction of a model active pharmaceutical with cationic surfactant and the subsequent design of drug based ionic liquid surfactants

Qamar, Sara; Brown, Paul; Ferguson, Steven; Khan, Rafaqat Ali; Ismail, Bushra; Khan, Abdur Rahman; Sayed, Murtaza; Khan, Asad Muhammad

doi:10.1016/j.jcis.2016.07.054

Cited by 33 publications

(12 citation statements)

References 33 publications

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“…Ionic liquids (ILs) are generally defined as organic salts with melting points below 100 • C [12][13][14]. They are usually composed of an organic cation and an inorganic/organic anion [15,16]. Inefficient crystal packing of the ions and/or a more diffuse charge on either or both ionic species leads to the weakening of the interactions between the cation and anion in ILs.…”

Section: Introductionmentioning

confidence: 99%

Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure

et al. 2019

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Lipid based formulations (LBFs) are commonly employed to enhance the absorption of highly lipophilic, poorly water-soluble drugs. However, the utility of LBFs can be limited by low drug solubility in the formulation. Isolation of ionizable drugs as low melting, lipophilic salts or ionic liquids (ILs) provides one means to enhance drug solubility in LBFs. However, whether different ILs benefit from formulation in different LBFs is largely unknown. In the current studies, lumefantrine was isolated as a number of different lipophilic salt/ionic liquid forms and performance was assessed after formulation in a range of LBFs. The solubility of lumefantrine in LBF was enhanced 2-to 80-fold by isolation as the lumefantrine docusate IL when compared to lumefantrine free base. The increase in drug loading subsequently enhanced concentrations in the aqueous phase of model intestinal fluids during in vitro dispersion and digestion testing of the LBF. To assess in vivo performance, the systemic exposure of lumefantrine docusate after administration in Type II-MCF, IIIB-MCF, IIIB-LCF, and IV formulations was evaluated after oral administration to rats. In vivo exposure was compared to control lipid and aqueous suspension formulations of lumefantrine free base. Lumefantrine docusate in the Type IIIB-LCF showed significantly higher plasma exposure compared to all other formulations (up to 35-fold higher). The data suggest that isolation of a lipid-soluble IL, coupled with an appropriate formulation, is a viable means to increase drug dose in an oral formulation and to enhance exposure of lumefantrine in vivo.

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Section: Introductionmentioning

confidence: 99%

Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure

et al. 2019

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“…Recently, there has been quite a few examples where nanotechnology was utilized to improve the efficiency of pharmaceutical by changing their drug delivery mechanism, or devising new drug delivery systems ,,. Liposomal, lipid and vesicles based, micellar, and polymers, NDs are some of the most commonly known forms of ND formulations …”

Section: Introductionmentioning

confidence: 99%

Structural Insights into the Microemulsion‐Mediated Formation of Fluoroquinolone Nanoantibiotics

et al. 2018

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Microemulsions (μEs) are being exploited as a potential route for yielding an extensive range of nanoparticles of different chemical nature, shapes and sizes. Nanodrugs offer new avenues for structuring better “drug delivery systems”. In this study, an oil‐in‐water (o/w) μE formulation comprising N‐butyl acetate/polysorbate 80/ethanol/water was developed for the preparation of nanoparticles of fluoroquinolone antibiotics (FLQ‐NPs). A pseudoternary phase diagram was mapped at constant surfactant/cosurfactant (1:2), revealing improved and high loading of FLQs in an optimum μE formulation. The as‐formulated μE showed high loading of FLQs as; levofloxacin (4.20 wt.%), ciprofloxacin (3.16 wt.%), moxifloxacin (2.53 wt.%), gatifloxacin (1.36 wt.%), ofloxacin (0.70 wt.%). Fourier transform IR analysis indicated good compatibility of each FLQ drug with μE excipients. However, dynamic light scattering showed an increase in the average particle size of the μE on drug loading, indicating the accumulation of FLQ at interface layer of the micelle. Additionally, lyophilized levofloxacin (a selected antibiotic) showed long‐term stability, amorphous morphology and improved dissolution rate, inspected by scanning transmission electron microscopy, X‐ray diffraction and electronic spectroscopy, respectively. Moreover, fluorescence measurements suggested the interfacial vicinity of levofloxacin within the μE domain, which may support controlled release of drug during systemic circulation.

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“…Such fitting inferences can be attributed to the addition of a non-ionic surfactant (polysorbate 80) and super disintegrates (crospovidone and SSG). The non-ionic surfactants (surfactants with an uncharged polar head group) are able to form micelle at a much lower concentration than ionic surfactants and have modifying effect on the rate of hydrolysis of drugs 18,19 , thus, enabling greater solubility. Furthermore, due to the uncharged nature, these surfactants are less sensitive to salt but quite sensitive to temperature.…”

Section: Determination Of Drugmentioning

confidence: 99%

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2020

IJPSR

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The aim of the current investigation was to develop bilayered immediate-release tablets of Telmisartan (TEL) and Hydrochlorothiazide (HCTZ) for the treatment of hypertension. In contrast to monotherapy, the dual drug therapy of TEL (an angiotensin II receptor blocker) and HCTZ (diuretic) is connoted to have a cumulative antihypertensive effect. Additionally, it offers ameliorative patient adherence to fixed-dose combination therapy over monotherapy and diminishes pill burden and dose-related side effects. The preformulation studies were accomplished by determining the compatibility of model drugs with their respective excipients by FTIR studies. These studies unambiguously connoted nix chemical interaction of excipients with the chosen model drugs. The formulation development was achieved in phases comprising of preliminary screening, pre-optimization and optimization studies. The wet granulation technique was adopted for formulating bilayer tablets. For preoptimization studies, five batches for each layer (T1-T5 for TEL and H1-H5 for HCTZ layer) were prepared. Based on the outcomes of pre-optimization, the formulation batches T2 and H5 were subsequently chosen for optimizing the varied process and formulation variables. The optimum bilayer formulation (T2H5) released drugs within 1 h (TEL-102.03% and HCTZ-101.03%) with individual layers. The super disintegrates attributing optimum immediate release characteristics were crospovidone (3.7% w/w) in TEL layer and sodium starch glycolate (1.66% w/w) in the HCTZ layer, respectively. The stability studies in conformity to ICH guidelines revealed a shelf life of 20 months. The study concluded that the bilayer tablets of TEL and HCTZ could be an alternative to a conventional dosage form for the treatment of hypertension. INTRODUCTION: A drug substance can be incorporated into numerous dosage forms for the convenient and efficacious treatment of a disease. The enteral routes are preferred by the majority of the patients in which the dosage form is to be swallowed and the absorption of the drug into bloodstream takes place through small intestine 1, 2 .

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The interaction of a model active pharmaceutical with cationic surfactant and the subsequent design of drug based ionic liquid surfactants

Cited by 33 publications

References 33 publications

Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure

Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure

Structural Insights into the Microemulsion‐Mediated Formation of Fluoroquinolone Nanoantibiotics

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