Solubility of LIDOCAINE in Ionic, Nonionic and Zwitterionic Surfactants

Ullah, Irfan; Baloch, Musa Kaleem; Durrani, Gulrez Fatima

doi:10.1007/s10953-012-9792-9

Cited by 18 publications

(8 citation statements)

References 28 publications

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“…The effectiveness of surfactant micelles on drug solubilization has been widely reported for a variety of surfactants . Many studies report the effects of the surfactant and drug chemical structure, electrolyte, and pH on the micellar solubilization of hydrophobic drugs. − Generally, for hydrophobic drugs, surfactants with nonionic headgroups are better solubilizing agents than ionic surfactants . Moreover, drug solubilization increases almost linearly with the increase of the hydrophobic chain length for neutral and charged surfactant types .…”

Section: Discussionmentioning

confidence: 99%

Mechanistic Investigation of Drug Supersaturation in the Presence of Polysorbates as Solubilizing Additives by Solution Nuclear Magnetic Resonance Spectroscopy

Arce

et al. 2021

Mol. Pharmaceutics

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The introduction of solubilizing additives has historically been an attractive approach to address the ever-growing proportion of poorly water-soluble drug (PWSD) compounds within the modern drug discovery pipeline. Lipid-formulations, and more specifically micelle formulations, have garnered particular interest because of their simplicity, size, scalability, and avoidance of solid-state limitations. Although micelle formulations have been widely utilized, the molecular mechanism of drug solubilization in surfactant micelles is still poorly understood. In this study, a series of modern nuclear magnetic resonance (NMR) methods are utilized to gain a molecular-level understanding of intermolecular interactions and kinetics in a model system. This approach enabled the understanding of how a PWSD, 17β-Estradiol (E2), solubilizes within a nonionic micelle system composed of polysorbate 80 (PS80). Based on one-dimensional (1D) 1 H chemical shift differences of E2 in PS80 solutions, as well as intermolecular correlations established from 1D selective nuclear Overhauser effect (NOE) and two-dimensional NOE spectroscopy experiments, E2 was found to accumulate within the palisade layer of PS80 micelles. A potential hydrogenbonding interaction between a hydroxyl group of E2 and a carbonyl group of PS80 alkane chains may allow for stabilizing E2−PS80 mixed micelles. Diffusion and relaxation NMR analysis and particle size measurements using dynamic light scattering indicate a slight increase in the micellar size with increasing degrees of supersaturation, resulting in slower mobility of the drug molecule. Based on these structural findings, a theoretical orientation model of E2 molecules with PS80 molecules was developed and validated by computational docking simulations.

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Section: Discussionmentioning

confidence: 99%

Mechanistic Investigation of Drug Supersaturation in the Presence of Polysorbates as Solubilizing Additives by Solution Nuclear Magnetic Resonance Spectroscopy

Arce

et al. 2021

Mol. Pharmaceutics

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“…Thermodynamics of micellization: Different thermodynamic parameters of micellization, the CMC, γCMC, πCMC, ∆Gmic, ∆Hmic and ∆Smic were plotted (Figs. [7][8][9][10] and listed in Table-1. It is clear that the critical micelle concentration of Brij58 (Fig.…”

Section: Critical Micelle Concentration and Thermodynamic Parametersmentioning

confidence: 99%

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mentioning

confidence: 99%

Applications of Different Techniques in Estimation of Aggregation and Thermodynamic Behaviour of Brij 58 at Different Temperatures

Niazi¹,

Durani²,

Baloch³

et al. 2014

Asian J. Chem.

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INTRODUCTIONA high percentage of pharmaceutically active compounds are insoluble in water having low and variable bioavailability 1,2 . Therefore, several techniques are in practice to increase the solubility of such drugs including the utility of the surfactants/ amphiphiles [3][4][5][6][7] . Surfactant are the substances that preferentially adsorb at an interface and lower the interfacial tension between two liquids or phases 8 . A large number of surfactants are available in the market, which have wide spread applications in different industries including dyestuffs, cosmetics, detergents, paints, plastic fibers, pesticides, pharmaceuticals and lubricants etc. 9 . The surface activity of surfactants is due to their amphiphilic structure having both a polar or hydrophilic head and a non-polar or a hydrophobic tail 10 . Their vital role in both fundamental and applied sciences is due to their most spectacular property to assemble into higher order structures spontaneously. This process is commonly known as self-assembly. It usually involves molecules that contain two distinct components, differing in their affinity for solutes. Molecules containing both hydrophobic and hydrophilic types of components with distinctive chemical and physical properties are said to be amphiphiles.An amphiphilic molecule can arrange itself at the surface of the water such that the polar part interacts with the water and the non-polar part is held above the surface (either in the air or in a non-polar liquid). The presence of these molecules

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“…1b) in which the tertiary amine is protonated (Ullah et al 2012;Rajabi et al 2011;Shaikh et al 2011). Therefore, lidocaine can be encapsulated or dispersed in a drug delivery vehicle which could be either hydrophobic or hydrophilic.…”

Section: Introductionmentioning

confidence: 99%

Potential of biodegradable microneedles as a transdermal delivery vehicle for lidocaine

Nayak

Das

2013

Biotechnol Lett

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There has been an increasing interest in applying biotechnology in formulating and characterising new and innovative drug delivery methods, e.g., drug-loaded biodegradable microneedles within the area of transdermal delivery technology. Recently, microneedles have been proposed for use in pain management, e.g., post-operative pain management through delivery of a local anaesthetic, namely, lidocaine. Lidocaine is a fairly common, marketed prescription-based local anaesthetic pharmaceutical, applied for relieving localised pain and lidocaine-loaded microneedles have been explored. The purpose of this review is to evaluate the properties of biodegradable polymers that may allow the preparation of microneedle systems, methods of preparing them and pharmacokinetic conditions in considering the potential use of lidocaine for delivery through the skin.

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Solubility of LIDOCAINE in Ionic, Nonionic and Zwitterionic Surfactants

Cited by 18 publications

References 28 publications

Mechanistic Investigation of Drug Supersaturation in the Presence of Polysorbates as Solubilizing Additives by Solution Nuclear Magnetic Resonance Spectroscopy

Mechanistic Investigation of Drug Supersaturation in the Presence of Polysorbates as Solubilizing Additives by Solution Nuclear Magnetic Resonance Spectroscopy

Applications of Different Techniques in Estimation of Aggregation and Thermodynamic Behaviour of Brij 58 at Different Temperatures

Potential of biodegradable microneedles as a transdermal delivery vehicle for lidocaine

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