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Pharmaceuticals
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Drug Delivery Systems for Local Anesthetics
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Drug Delivery Systems for Local Anesthetics

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (22 August 2024) | Viewed by 5815

Special Issue Editors

Prof. Dr. Michelle Franz-Montan

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Guest Editor
Department of Biosciences, Piracicaba Dental School, University of Campinas (UNICAMP), Piracicaba 13083-970, SP, Brazil
Interests: topical anesthesia; oral cavity; oral mucosa; dental anesthesia; drug delivery; mucoadhesive system; dentistry
Special Issues, Collections and Topics in MDPI journals
Dr. Camila Batista Da Silva

E-Mail Website
Guest Editor
Department of Biosciences, Piracicaba Dental School, Universidade Estadual de Campinas, Sao Paulo, Brazil
Interests: dentistry; anesthesia; local anesthesia; anxiety; pain; drug delivery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Local anesthetics (LAs) are among the most useful drugs in anesthesiology practice and pain management, as they cause a temporary loss of pain by inhibiting the transmission of nerve impulses. Thus, they have been widely used in clinical practice. However, the applications of anesthetics are greatly limited due to their neurotoxicity and short half-lives. To overcome these barriers, numerous drug delivery systems (DDSs) have been designed to encapsulate local anesthetic agents so that large doses can be released slowly and provide analgesia over a prolonged period. Formulation approaches to systemically deliver LA include the encapsulation of liposomes, the complexation of cyclodextrins, and associations with biopolymers and other carrier systems. This Special Issue, entitled “Drug Delivery Systems for Local Anesthetics”, considers drug delivery formulations of local anesthetics designed to prolong the anesthetic effect and decrease toxicity.

We invite authors to submit original research articles or review articles outlining innovations pertaining to formulations and techniques for drug delivery of topical and injectable local anesthetics.

Prof. Dr. Michelle Franz-Montan
Dr. Camila Batista Da Silva
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • local anesthetics
  • drug delivery system
  • liposomes
  • biopolymers
  • cyclodextrins
  • polymers
  • micro- and nanoparticles
  • topical formulations

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Published Papers (3 papers)

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Research

16 pages, 995 KiB  
Article
Extended Release of Bupivacaine from Temperature-Responsive PNDJ Hydrogels Improves Postoperative Weight-Bearing in Rabbits Following Knee Surgery
by Derek J. Overstreet, Gabriel Zdrale and Alex C. McLaren
Pharmaceuticals 2024, 17(7), 879; https://doi.org/10.3390/ph17070879 - 3 Jul 2024
Cited by 2 | Viewed by 1468
Abstract
Effective treatment of postoperative pain lasting for multiple days without opioids is an important clinical need. We previously reported analgesia lasting up to 96 h in a porcine soft tissue model of postoperative pain using SBG004, an extended-release formulation of bupivacaine based on [...] Read more.
Effective treatment of postoperative pain lasting for multiple days without opioids is an important clinical need. We previously reported analgesia lasting up to 96 h in a porcine soft tissue model of postoperative pain using SBG004, an extended-release formulation of bupivacaine based on the temperature-responsive polymer poly(N-isopropylacrylamide-co-dimethylbutyrolactone acrylamide-co-Jeffamine M-1000 acrylamide) [PNDJ]. Orthopaedic surgical sites such as the knee can involve complex sensory innervation which presents a distinct challenge to local anesthetic delivery. The purpose of this work was to evaluate the pharmacokinetics and efficacy of SBG004 in an orthopaedic surgical model in comparison to currently available local anesthetics. Pharmacokinetics following periarticular (PA) or intraarticular (IA) injection of SBG004 were compared against liposomal bupivacaine (Lip-Bupi) PA in New Zealand White rabbits (all doses 14.5 mg/kg). Analgesic efficacy of SBG004 (IA, PA, or IA + PA), three active comparators, and saline was evaluated following knee surgery in New Zealand White rabbits. Analgesia was assessed via weight-bearing on the operated limb during spontaneous large steps in video recordings. Systemic bupivacaine exposure lasted at least 7 days for SBG004 PA, 4 days for SBG004 IA, and 2 days for Lip-Bupi PA. In the analgesia study, weight-bearing in all active groups except SBG004 IA was more frequent versus saline through 8 h postoperatively (p < 0.05). Only SBG004 IA + PA resulted in a higher proportion of weight-bearing rabbits at 24 h versus saline (6/7 versus 2/10, p = 0.015). Analysis of pooled data from 24–72 h showed significantly greater frequency of weight-bearing in rabbits receiving SBG004 IA + PA (71%) versus saline (37%), ropivacaine cocktail (41%), and Lip-Bupi PA (36%). The results indicate that the release profile from SBG004 PA or IA coincides reasonably with the time course of postoperative pain, and SBG004 may produce longer duration of analgesia than local anesthetics currently used in knee surgery, including during the period of 24–72 h recognized as a target for extended-release local anesthetics. Full article
(This article belongs to the Special Issue Drug Delivery Systems for Local Anesthetics)
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14 pages, 2036 KiB  
Article
Polymeric Nanocapsules Loaded with Lidocaine: A Promising Formulation for Topical Dental Anesthesia
by Camila Batista da Silva, Cleiton Pita dos Santos, Luciano Serpe, Jonny Burga Sanchez, Luiz Eduardo Nunes Ferreira, Nathalie Ferreira Silva de Melo, Francisco Carlos Groppo, Leonardo Fernandes Fraceto, Maria Cristina Volpato and Michelle Franz-Montan
Pharmaceuticals 2024, 17(4), 485; https://doi.org/10.3390/ph17040485 - 10 Apr 2024
Cited by 3 | Viewed by 1963
Abstract
Lidocaine is the most commonly used local anesthetic worldwide, known for its rapid onset and moderate duration of anesthesia. However, it is short-lived and does not effectively promote effective topical anesthesia in the oral cavity when used alone. Our aim was to investigate [...] Read more.
Lidocaine is the most commonly used local anesthetic worldwide, known for its rapid onset and moderate duration of anesthesia. However, it is short-lived and does not effectively promote effective topical anesthesia in the oral cavity when used alone. Our aim was to investigate whether an approximate 50% encapsulation of lidocaine in poly(ε-caprolactone) nanocapsules (LDC-Nano) would be able to increase its permeation and analgesic efficacy and reduce cytotoxicity. In this study, we characterized LDC-Nano and conducted MTT tests with HaCaT cells to assess their in vitro cytotoxicity. Additionally, in vitro permeation assays across the pig esophageal epithelium and the anesthetic efficacy of the hind paw incision model in rats were performed. Plain lidocaine (LDC) was compared with LDC-Nano and lidocaine hydrochloride plus epinephrine (LDC-Epi). The physicochemical characteristics of LDC-Nano were satisfactory (pH: 8.1 ± 0.21; polydispersity index: 0.08 ± 0.01; mean diameter (nm): 557.8 ± 22.7; and encapsulation efficiency (%): 51.8 ± 1.87) and remained stable for up to 4 months. LDC-Nano presented similar in vitro cytotoxicity to LDC but was higher than LDC-Epi (LD50: LDC = 0.48%; LDC-Nano = 0.47%; and LDC-Epi = 0.58%; p < 0.0001). Encapsulation increased the permeability coefficient about 6.6 times and about 7.5 the steady-state flux of lidocaine across the mucosal epithelium. Both encapsulation and epinephrine improved anesthesia duration, with epinephrine demonstrating superior efficacy (100% of animals were anesthetized up to 100, 30, and 20 min when LDC-Epi, LDC-nano, and LDC were used, respectively). Although LDC-Epi demonstrated superior in vivo anesthetic efficacy, the in vitro permeation and cytotoxicity of LDC-Nano indicate promising avenues for future research, particularly in exploring its potential application as a topical anesthetic in the oral cavity. Full article
(This article belongs to the Special Issue Drug Delivery Systems for Local Anesthetics)
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12 pages, 1944 KiB  
Article
Development of a Dosage form for a Photoswitchable Local Anesthetic Ethercaine
by Alexey Noev, Natalia Morozova, Nikita Suvorov, Yuriy Vasil’ev, Andrei Pankratov and Mikhail Grin
Pharmaceuticals 2023, 16(10), 1398; https://doi.org/10.3390/ph16101398 - 2 Oct 2023
Cited by 5 | Viewed by 1763
Abstract
The toxicity of local anesthetics is a serious problem, given their widespread use. One of the main causes of the side effects of local anesthetics is their non-selectivity of action in the body. A possible way to increase the selectivity of the action [...] Read more.
The toxicity of local anesthetics is a serious problem, given their widespread use. One of the main causes of the side effects of local anesthetics is their non-selectivity of action in the body. A possible way to increase the selectivity of the action of drugs is to use the photopharmacology approach. Previously, we described the light-controlled local anesthetic ethercaine, the biological effect of which can be controlled using light, thereby increasing its selectivity of action. An important limitation of ethercaine was its low solubility in water, limiting the potential of this compound. In this work, we developed a dosage form of ethercaine, which allowed us to increase its solubility from 0.6% to 2% or more. The resulting 1% solution of ethercaine hydrochloride in 4% Kolliphor ELP had high biological activity on the surface anesthesia model, while demonstrating low acute toxicity in mice with intravenous administration (4–5 times less than that of lidocaine). Full article
(This article belongs to the Special Issue Drug Delivery Systems for Local Anesthetics)
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