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Pharmaceutics
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Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics
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Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (15 August 2021) | Viewed by 14545

Special Issue Editors

Prof. Dr. Eneida de Paula

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Guest Editor
Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas—UNICAMP, Campinas 13083-862, SP, Brazil
Interests: drug delivery; lipid nanoparticles; nanocarriers; local anesthetics; anti-inflammatory
Special Issues, Collections and Topics in MDPI journals
Dr. Lígia N.M. Ribeiro

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Guest Editor
Institute of Biotechnology, Federal University of Uberlandia, Uberlandia 38408-100, MG, Brazil
Interests: drug delivery; nanomaterials characterization; natural excipients; nanocolloids; hybrid formulations
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The local anesthesia procedure in medical and veterinary routine is employed to minimize and/or prevent painful symptoms of patients. However, local anesthetics (LA) molecules cause important systemic effects on the cardiovascular system. Therefore, LA must be administered with parsimony, decreasing their anesthesia duration. There is still a lack of pharmaceutical dosage forms that can improve the antinociceptive effect while reducing LA toxicity. The development of lipid-based drug delivery systems (LDDS) is a versatile approach aiming at long-term analgesia with immediate onset, decreasing LA toxicity. LDDS, such as liposomes, nanoemulsions, nanostructured lipid carriers, solid lipid nanoparticles, lipid nanocapsules, and lipid-based hybrid formulations can act as promising matrices to provide novel LDDS for LA delivery. Nanotechnological innovations and therapies, as well as the challenges to be overcome, mainly related to scaling up, economic viability, and preclinical and clinical efficacy assays, should also be also discussed.

Prof. Dr. Eneida de Paula
Dr. Lígia N.M. Ribeiro
Guest Editors

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Keywords

  • local anesthetics
  • drug delivery
  • lipid nanoparticles
  • liposomes
  • lipid nanocapsules
  • nanoemulsions
  • lipid–polymer formulations
  • topical anesthesia
  • infiltrative anesthesia
  • local anesthetics candidate drugs
  • in vitro characterization methods
  • in vivo antinociceptive assays

Published Papers (5 papers)

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16 pages, 1698 KiB  
Article
Mucoadhesive, Thermoreversible Hydrogel, Containing Tetracaine-Loaded Nanostructured Lipid Carriers for Topical, Intranasal Needle-Free Anesthesia
by Giovana Maria Fioramonti Calixto, Bruno Vilela Muniz, Simone R. Castro, Jaiza Samara Macena de Araujo, Klinger de Souza Amorim, Lígia N. M. Ribeiro, Luiz Eduardo Nunes Ferreira, Daniele Ribeiro de Araújo, Eneida de Paula and Michelle Franz-Montan
Pharmaceutics 2021, 13(11), 1760; https://doi.org/10.3390/pharmaceutics13111760 - 21 Oct 2021
Cited by 9 | Viewed by 2678
Abstract
Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained [...] Read more.
Recent advances have been reported for needle-free local anesthesia in maxillary teeth by administering a nasal spray of tetracaine (TTC) and oxymetazoline, without causing pain, fear, and stress. This work aimed to assess whether a TTC-loaded hybrid system could reduce cytotoxicity, promote sustained permeation, and increase the anesthetic efficacy of TTC for safe, effective, painless, and prolonged analgesia of the maxillary teeth in dental procedures. The hybrid system based on TTC (4%) encapsulated in nanostructured lipid carriers (NLC) and incorporated into a thermoreversible hydrogel of poloxamer 407 (TTCNLC-HG4%) displayed desirable rheological, mechanical, and mucoadhesive properties for topical application in the nasal cavity. Compared to control formulations, the use of TTCNLC-HG4% slowed in vitro permeation of the anesthetic across the nasal mucosa, maintained cytotoxicity against neuroblastoma cells, and provided a three-fold increase in analgesia duration, as observed using the tail-flick test in mice. The results obtained here open up perspectives for future clinical evaluation of the thermoreversible hybrid hydrogel, which contains TTC-loaded NLC, with the aim of creating an effective, topical, intranasal, needle-free anesthesia for use in dentistry. Full article
(This article belongs to the Special Issue Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics)
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25 pages, 5530 KiB  
Article
Docetaxel and Lidocaine Co-Loaded (NLC-in-Hydrogel) Hybrid System Designed for the Treatment of Melanoma
by Ludmilla David de Moura, Lígia N. M. Ribeiro, Fabíola V. de Carvalho, Gustavo H. Rodrigues da Silva, Priscila C. Lima Fernandes, Sérgio Q. Brunetto, Celso D. Ramos, Lício A. Velloso, Daniele R. de Araújo and Eneida de Paula
Pharmaceutics 2021, 13(10), 1552; https://doi.org/10.3390/pharmaceutics13101552 - 24 Sep 2021
Cited by 18 | Viewed by 3335
Abstract
Melanoma is the most aggressive skin carcinoma and nanotechnology can bring new options for its pharmacological treatment. Nanostructured lipid carriers (NLC) are ideal drug-delivery carriers for hydrophobic drugs, such as the antineoplastic docetaxel (DTX), and hybrid (NLC-in-hydrogel) systems are suitable for topical application. [...] Read more.
Melanoma is the most aggressive skin carcinoma and nanotechnology can bring new options for its pharmacological treatment. Nanostructured lipid carriers (NLC) are ideal drug-delivery carriers for hydrophobic drugs, such as the antineoplastic docetaxel (DTX), and hybrid (NLC-in-hydrogel) systems are suitable for topical application. This work describes a formulation of NLCDTX in xanthan-chitosan hydrogel containing lidocaine (LDC) with anticancer and analgesia effects. The optimized nanoparticles encapsulated 96% DTX and rheological analysis revealed inherent viscoelastic properties of the hydrogel. In vitro assays over murine fibroblasts (NIH/3T3) and melanoma cells (B16-F10), human keratinocytes (HaCaT) and melanoma cells (SK-MEL-103) showed reduction of docetaxel cytotoxicity after encapsulation in NLCDTX and HGel-NLCDTX. Addition of LDC to the hybrid system (HGel-NLCDTX-LDC) increased cell death in tumor and normal cells. In vivo tests on C57BL/6J mice with B16-F10-induced melanoma indicated that LDC, NLCDTX, HGel-NLCDTX-LDC and NLCDTX + HGel-LDC significantly inhibited tumor growth while microPET/SPECT/CT data suggest better prognosis with the hybrid treatment. No adverse effects were observed in cell survival, weight/feed-consumption or serum biochemical markers (ALT, AST, creatinine, urea) of animals treated with NLCDTX or the hybrid system. These results confirm the adjuvant antitumor effect of lidocaine and endorse HGel-NLCDTX-LDC as a promising formulation for the topical treatment of melanoma. Full article
(This article belongs to the Special Issue Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics)
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18 pages, 4148 KiB  
Article
Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery
by Ji-Hyun Kang, Kwang-Hwi Yoo, Hyo-Young Park, Seung-Min Hyun, Sang-Duk Han, Dong-Wook Kim and Chun-Woong Park
Pharmaceutics 2021, 13(9), 1468; https://doi.org/10.3390/pharmaceutics13091468 - 14 Sep 2021
Cited by 12 | Viewed by 3574 | Correction
Abstract
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 [...] Read more.
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. Full article
(This article belongs to the Special Issue Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics)
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17 pages, 1922 KiB  
Article
Liposomal Bupivacaine (Bupigel) Demonstrates Minimal Local Nerve Toxicity in a Rabbit Functional Model
by Yaelle Bavli, Malcolm Rabie, Yakov Fellig, Yoram Nevo and Yechezkel Barenholz
Pharmaceutics 2021, 13(2), 185; https://doi.org/10.3390/pharmaceutics13020185 - 1 Feb 2021
Cited by 4 | Viewed by 2759
Abstract
We previously reported the development of a novel formulation of an ultra-long-acting local anesthetic based on bupivacaine encapsulated in large multivesicular liposomes (Bupisomes) embedded in hydrogel. This formulation (Bupigel) prolonged bupivacaine release from the formulation in dissolution-like studies in vitro and analgesia in [...] Read more.
We previously reported the development of a novel formulation of an ultra-long-acting local anesthetic based on bupivacaine encapsulated in large multivesicular liposomes (Bupisomes) embedded in hydrogel. This formulation (Bupigel) prolonged bupivacaine release from the formulation in dissolution-like studies in vitro and analgesia in vivo in mouse, rat, and pig models. In this study we assessed Bupigel neurotoxicity on rabbit sciatic nerve using histopathology and electrophysiologic testing. Sciatic nerves of both hind limbs were injected dropwise with different formulations. Nerve conduction studies and needle electromyography two weeks after perineural administration showed signs of neural damage after injection of free lidocaine and bupivacaine, while there was no sign of neural damage after injection with saline, demonstrating the validity of the method. This test also did not show evidence of motor or sensory nerve damage after injection with liposomal bupivacaine at a dose 10-times higher than free bupivacaine. Histologically, signs of neural damage could be observed with lidocaine. Nerves injected with Bupigel showed mild signs of inflammation and small residues of hydrogel in granulomas, indicating a long residence time of the hydrogel at the site of injection, but no histopathological signs of nerve damage. This demonstrated that early signs of neural damage were detected electrophysiologically, showing the usefulness and sensitivity of electrodiagnostic testing in detection of neural damage from new formulations. Full article
(This article belongs to the Special Issue Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics)
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2 pages, 630 KiB  
Correction
Correction: Kang et al. Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery. Pharmaceutics 2021, 13, 1468
by Ji-Hyun Kang, Kwang-Hwi Yoo, Hyo-Young Park, Seung-Min Hyun, Sang-Duk Han, Dong-Wook Kim and Chun-Woong Park
Pharmaceutics 2022, 14(1), 155; https://doi.org/10.3390/pharmaceutics14010155 - 10 Jan 2022
Viewed by 1073
Abstract
The authors wish to make the following corrections to this paper [...] Full article
(This article belongs to the Special Issue Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics)
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