Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

López‐Iglesias, Clara; Quílez, Cristina; Barros, Joana; Velasco, Diego; Alvarez‐Lorenzo, Carmen; Jorcano, José L.; Monteiro, Fernando J.; García‐González, Carlos A.

doi:10.3390/pharmaceutics12090870

Cited by 22 publications

(9 citation statements)

References 62 publications

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“…The thermogram of GMS and lidocaine showed a sharp endothermic peak at 65 °C and 70 °C, which was indicative of the melting and crystalline nature of GMS and lidocaine. This is similar to the previously reported melting temperature (Tm) values of GMS and lidocaine [ 48 ]. The thermogram of the L2 and L3 ointment, made with 5% and 10% GMS, showed a widened and split endothermic peak from 50 °C to 60 °C.…”

Section: Resultssupporting

confidence: 91%

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

et al. 2021

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Lidocaine, a commonly used local anesthetic, has recently been developed into a number of ointment products to treat hemorrhoids. This study examined its efficient delivery to the dermis through the pharmaceutical improvement of hemorrhoid treatment ointments. We attempted to increase the amount of skin deposition of lidocaine by forming a nanoemulsion through the self-nanoemulsifying effect that occurs when glycerol monostearate (GMS) is saturated with water. Using Raman mapping, the depth of penetration of lidocaine was visualized and confirmed, and the local anesthetic effect was evaluated via an in vivo tail-flick test. Evaluation of the physicochemical properties confirmed that lidocaine was amorphous and evenly dispersed in the ointment. The in vitro dissolution test confirmed that the nanoemulsifying effect of GMS accelerated the release of the drug from the ointment. At a specific concentration of GMS, lidocaine penetrated deeper into the dermis; the in vitro permeation test showed similar results. When compared with reference product A in the tail-flick test, the L5 and L6 compounds containing GMS had a significantly higher anesthetic effect. Altogether, the self-nanoemulsifying effect of GMS accelerated the release of lidocaine from the ointment. The compound with 5% GMS, the lowest concentration that saturated the dermis, was deemed most appropriate.

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Section: Resultssupporting

confidence: 91%

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

et al. 2021

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“…NPs Inorganic NPs Metal nanoparticles: CuNPs, 87 AgNPs, 88,89 and Cerium Oxide NPs 90 Carbon-based NPs 91,92 Quantum dots: self-assembled GQDs, 93 Orange-emissive carbon quantum dots 94 Organic NPs Dendrimers: act as antibacterial agents 95,96 Hydrogels: chitosan, 97 PVA, 98 and PEG 99 Nano-emulsions can improve the solubility and reduce the enzymatic hydrolysis of drugs 100 Liposomal NPs: solid lipid NPs 101,102 and nanostructured lipid carriers 103,104 Polymer NPs PCL, 69 PEG, 68 and photothermal NPs 105 Smart stimuli-responsive nanostructures MMP9-responsive, 106 pH-responsive, 107 immune responsive, 72 and thermosensitive nanostructures 99 Nanofibers (NFs) NFs can increase the transfer of various molecules and perform diverse functions 108 Microspheres coated with nanocomposites PCL microspheres, 86 chitin microspheres, 109 bacterial cellulose microspheres, 110 and gelatin microspheres 111 3D-printed scaffolds Typical three-dimensional porous matrix 112 Engineered films Agar-glycerol-sericin films 113,114 Abbreviations: GQD, graphene quantum dots; MMP, matrix metalloproteinase.…”

Section: Category Examplesmentioning

confidence: 99%

Nanobiotechnology: Applications in Chronic Wound Healing

Jiang¹,

Li²,

Qiu³

et al. 2022

IJN

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Wounds occur when skin integrity is broken and the skin is damaged. With progressive changes in the disease spectrum, the acute wounds caused by mechanical trauma have been become less common, while chronic wounds triggered with aging, diabetes and infection have become more frequent. Chronic wounds now affect more than 6 million people in the United States, amounting to 10 billion dollars in annual expenditure. However, the treatment of chronic wounds is associated with numerous challenges. Traditional remedies for chronic wounds include skin grafting, flap transplantation, negative-pressure wound therapy, and gauze dressing, all of which can cause tissue damage or activity limitations. Nanobiotechnology — which comprises a diverse array of technologies derived from engineering, chemistry, and biology — is now being applied in biomedical practice. Here, we review the design, application, and clinical trials for nanotechnology-based therapies for chronic wound healing, highlighting the clinical potential of nanobiotechnology in such treatments. By summarizing previous nanobiotechnology studies, we lay the foundation for future wound care via a nanotech-based multifunctional smart system.

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“…To determine the selecting, the most appropriate model for predicting the mechanism of drug release, the dissolution profiles of all batches were fitted to zeroorder [1], first-order [2], Higuchi [3], Hixson-Crowell [4], and Korsmeyer-Peppas [5] kinetic models. 26…”

Section: Kinetic Modeling Of Drug Releasementioning

confidence: 99%

“…2 Solid lipid microparticles have a better physicochemical stability than other lipid-based drug carriers, such as liposomes, and are easier to sterilize and scale-up. 3 The formulation of solid lipid microparticles (SLMs) for effective oral administration of biological medicines begins with the selection of appropriate lipid excipients with the right hydrophobicity and lipolysis propensity. 4 Zidovudine is a synthetic nucleoside analogue that is increasingly being employed as the cornerstone of antiretroviral therapy for HIV infection.…”

Section: Introductionmentioning

confidence: 99%

Utility of Different Lipids and Effect of Soya Lecithin on Sustained Delivery of Zidovudine via Biodegradable Solid Lipid Microparticles: Formulation and in-vitro Characterization

Sathyamoorthy¹,

Sundar²,

Rajendran³

et al. 2022

IJPER

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Background: Zidovudine (Azidothymidine, AZT) is widely used in the treatment of Acquired Immuno Deficiency Syndrome (AIDS) and related conditions, either alone or in combination with other antiviral agents to combat HIV. AZT is a Biopharmaceutical Classification System (BCS) class III drug and has various disadvantages. Thus, AZT is a potential candidate for delivery via lipid-based drug delivery system. Materials and Methods: In the present work, solid lipid microparticles (SLMs) of Zidovudine were developed for sustaining the drug release, to overcome or to reduce the hepatic metabolism and to ensure optimal bioavailability. A total of sixteen formulations of Zidovudine loaded solid lipid microparticles in two groups viz., one with tripalmitin and another with trimyristin were prepared by emulsion-solvent evaporation method. Results: The average particle size and entrapment efficiency of the prepared SLM varied between 5.48 µm-10.64 µm and 46.92 % and 58.39% respectively. The release of zidovudine from the SLM varied between 70.47% and 100% at the end of 24 hrs. 80% of the drug release which is required for obtaining the optimal therapeutic concentration was achieved by SLM 8. Conclusion: Formulation SLM 8 was considered best with maximum sustainability in the drug release along with maintaining therapeutic optimum. The formulation was found stable under stressed conditions.

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Lidocaine-Loaded Solid Lipid Microparticles (SLMPs) Produced from Gas-Saturated Solutions for Wound Applications

Cited by 22 publications

References 62 publications

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

Nanobiotechnology: Applications in Chronic Wound Healing

Utility of Different Lipids and Effect of Soya Lecithin on Sustained Delivery of Zidovudine via Biodegradable Solid Lipid Microparticles: Formulation and in-vitro Characterization

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