Lipid nanoparticles for topical and transdermal delivery of pharmaceuticals and cosmeceuticals

Sengar, Vaishali; Jyoti, Kiran; Jain, Upendra Kumar; Katare, Om Prakash; Chandra, Ramesh; Madan, Jitender

doi:10.1016/b978-0-12-813687-4.00010-4

Cited by 4 publications

(3 citation statements)

References 78 publications

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“…The optimized pharmacokinetic and biological properties of LA-loaded SLNs have been reported for lidocaine, prilocaine, bupivacaine, and articaine [7,10,11,12]. In light of this, we considered encapsulating DBC in SLNs to enhance its bioavailability and to minimize its systemic toxicity [13,14].…”

Section: Introductionmentioning

confidence: 99%

Solid Lipid Nanoparticles for Dibucaine Sustained Release

et al. 2018

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Dibucaine (DBC) is among the more potent long-acting local anesthetics (LA), and it is also one of the most toxic. Over the last decades, solid lipid nanoparticles (SLN) have been developed as promising carriers for drug delivery. In this study, SLN formulations were prepared with the aim of prolonging DBC release and reducing its toxicity. To this end, SLN composed of two different lipid matrices and prepared by two different hot-emulsion techniques (high-pressure procedure and sonication) were compared. The colloidal stability of the SLN formulations was tracked in terms of particle size (nm), polydispersity index (PDI), and zeta potential (mV) for 240 days at 4 °C; the DBC encapsulation efficiency was determined by the ultrafiltration/centrifugation method. The formulations were characterized by differential scanning calorimetry (DSC), electron paramagnetic resonance (EPR), and release kinetic experiments. Finally, the in vitro cytotoxicity against 3T3 fibroblast and HaCaT cells was determined, and the in vivo analgesic action was assessed using the tail flick test in rats. Both of the homogenization procedures were found suitable to produce particles in the 200 nm range, with good shelf stability (240 days) and high DBC encapsulation efficiency (~72–89%). DSC results disclosed structural information on the nanoparticles, such as the lower crystallinity of the lipid core vs. the bulk lipid. EPR measurements provided evidence of DBC partitioning in both SLNs. In vitro (cytotoxicity) and in vivo (tail flick) experiments revealed that the encapsulation of DBC into nanoparticles reduces its intrinsic cytotoxicity and prolongs the anesthetic effect, respectively. These results show that the SLNs produced are safe and have great potential to extend the applications of dibucaine by enhancing its bioavailability.

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Section: Introductionmentioning

confidence: 99%

Solid Lipid Nanoparticles for Dibucaine Sustained Release

et al. 2018

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“…The inclusion of active pharmaceutical ingredients in drug delivery systems is the contemporary approach to overcome problems such as poor solubility, stability, and permeation [44][45][46]. Indisputably, lipid-based nanoparticles are among the most attractive drug carriers in the field of dermal and transdermal drug delivery [47,48]. This is in compliance with their structural similarity to skin barriers and compatibility with the majority of dermal bases.…”

Section: Introductionmentioning

confidence: 99%

“…Depending on the nature of the lipids, the experimental conditions, and the ingredients ratio, nanosized aggregates may occur with different morphology, from liquid core-elastic wall vesicles (liposomes, niosomes, ethosomes) to thermodynamically stable liquid-in-liquid systems (nanoemulsions) or variously structured solid or soft particles (solid lipid nanoparticles or other types of nanostructured lipid carriers). However, all of the above-mentioned lipid-based nanocarriers possess some universal features, such as the ability to modify drug release, encapsulate efficiently hydrophobic molecules (and some hydrophilic ones, as well), improve drug solubility and permeation, and increase drug stability by providing a protective microenvironment [47][48][49]. As the lipid-based nanotechnologies often involve steps in preparation at higher temperatures and/or sonication [50], the chemical stability of the active compounds under such conditions should be investigated and considered.…”

Section: Introductionmentioning

confidence: 99%

Dermal Drug Delivery of Phytochemicals with Phenolic Structure via Lipid-Based Nanotechnologies

et al. 2021

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Phenolic compounds are a large, heterogeneous group of secondary metabolites found in various plants and herbal substances. From the perspective of dermatology, the most important benefits for human health are their pharmacological effects on oxidation processes, inflammation, vascular pathology, immune response, precancerous and oncological lesions or formations, and microbial growth. Because the nature of phenolic compounds is designed to fit the phytochemical needs of plants and not the biopharmaceutical requirements for a specific route of delivery (dermal or other), their utilization in cutaneous formulations sets challenges to drug development. These are encountered often due to insufficient water solubility, high molecular weight and low permeation and/or high reactivity (inherent for the set of representatives) and subsequent chemical/photochemical instability and ionizability. The inclusion of phenolic phytochemicals in lipid-based nanocarriers (such as nanoemulsions, liposomes and solid lipid nanoparticles) is so far recognized as a strategic physico-chemical approach to improve their in situ stability and introduction to the skin barriers, with a view to enhance bioavailability and therapeutic potency. This current review is focused on recent advances and achievements in this area.

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