Sustained release local anesthetics for pain management: relevance and formulation approaches
This review attempted to ascertain the rationale for the formulation of sustained-release local anesthetics and summarize the various formulation approaches designed to date to achieve sustained and localized local analgesic effects. The incidence of pain, which is the concern of patients as well as...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2024-04-01
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| Series: | Frontiers in Pain Research |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fpain.2024.1383461/full |
| _version_ | 1797221866993090560 |
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| author | Melese Getachew Hana Tesfaye Wubetu Yihunie Tesfahun Ayenew Sintayehu Alemu Ephrem Mebratu Dagnew Yalemgeta Biyazin Dehnnet Abebe Natanim Degefu Abtie Abebaw |
| author_facet | Melese Getachew Hana Tesfaye Wubetu Yihunie Tesfahun Ayenew Sintayehu Alemu Ephrem Mebratu Dagnew Yalemgeta Biyazin Dehnnet Abebe Natanim Degefu Abtie Abebaw |
| author_sort | Melese Getachew |
| collection | DOAJ |
| description | This review attempted to ascertain the rationale for the formulation of sustained-release local anesthetics and summarize the various formulation approaches designed to date to achieve sustained and localized local analgesic effects. The incidence of pain, which is the concern of patients as well as health care professionals, is increasing due to accidents, surgical procedures, and other diseases. Local anesthetics can be used for the management of moderate to severe acute and chronic pain. They also allow regional analgesia, in situations where the cause and source of the pain are limited to a particular site or region, without the need for loss of consciousness or systemic administration of other analgesics thereby decreasing the risk of potential toxicities. Though they have an interesting antipain efficacy, the short duration of action of local anesthetics makes the need for their multiple injections or opioid adjuvants mandatory. To overcome this problem, different formulations are being designed that help achieve prolonged analgesia with a single dose of administration. Combination with adjuvants, liposomal formulations, lipid-based nanoparticles, thermo-responsive nanogels, microspheres, microcapsules, complexation with multivalent counterions and HP-β-CD, lipid-based nanoparticles, and bio-adhesive films, and polymeric matrices are among the approaches. Further safety studies are required to ensure the safe and effective utilization of sustained-release local anesthetics. Moreover, the release kinetics of the various formulations should be adequately established. |
| first_indexed | 2024-04-24T13:12:15Z |
| format | Article |
| id | doaj.art-eb0adde04a4446209a9c7826c4229923 |
| institution | Directory Open Access Journal |
| issn | 2673-561X |
| language | English |
| last_indexed | 2024-04-24T13:12:15Z |
| publishDate | 2024-04-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pain Research |
| spelling | doaj.art-eb0adde04a4446209a9c7826c42299232024-04-05T04:35:22ZengFrontiers Media S.A.Frontiers in Pain Research2673-561X2024-04-01510.3389/fpain.2024.13834611383461Sustained release local anesthetics for pain management: relevance and formulation approachesMelese Getachew0Hana Tesfaye1Wubetu Yihunie2Tesfahun Ayenew3Sintayehu Alemu4Ephrem Mebratu Dagnew5Yalemgeta Biyazin6Dehnnet Abebe7Natanim Degefu8Abtie Abebaw9Department of Pharmacy, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaSchool of Pharmacy, College of Medicine and Health Sciences, University of Gondar, Gondar, EthiopiaDepartment of Pharmacy, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaDepartment of Nursing, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaDepartment of Pharmaceutics, School of Pharmacy, Institute of Health, Jimma University, Jimma, EthiopiaDepartment of Pharmacy, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaDepartment of Pediatrics and Child Health Nursing, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaDepartment of Pharmacy, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaDepartment of Pharmaceutics, School of Pharmacy, College of Health and Medical Sciences, Haramaya University, Harar, EthiopiaDepartment of Medical Laboratory Sciences, College of Medicine and Health Sciences, Debre Markos University, Debre Markos, EthiopiaThis review attempted to ascertain the rationale for the formulation of sustained-release local anesthetics and summarize the various formulation approaches designed to date to achieve sustained and localized local analgesic effects. The incidence of pain, which is the concern of patients as well as health care professionals, is increasing due to accidents, surgical procedures, and other diseases. Local anesthetics can be used for the management of moderate to severe acute and chronic pain. They also allow regional analgesia, in situations where the cause and source of the pain are limited to a particular site or region, without the need for loss of consciousness or systemic administration of other analgesics thereby decreasing the risk of potential toxicities. Though they have an interesting antipain efficacy, the short duration of action of local anesthetics makes the need for their multiple injections or opioid adjuvants mandatory. To overcome this problem, different formulations are being designed that help achieve prolonged analgesia with a single dose of administration. Combination with adjuvants, liposomal formulations, lipid-based nanoparticles, thermo-responsive nanogels, microspheres, microcapsules, complexation with multivalent counterions and HP-β-CD, lipid-based nanoparticles, and bio-adhesive films, and polymeric matrices are among the approaches. Further safety studies are required to ensure the safe and effective utilization of sustained-release local anesthetics. Moreover, the release kinetics of the various formulations should be adequately established.https://www.frontiersin.org/articles/10.3389/fpain.2024.1383461/fullchronic painformulation approachesliposomal formulationslipid nanoparticleslocal anestheticslocalized analgesia |
| spellingShingle | Melese Getachew Hana Tesfaye Wubetu Yihunie Tesfahun Ayenew Sintayehu Alemu Ephrem Mebratu Dagnew Yalemgeta Biyazin Dehnnet Abebe Natanim Degefu Abtie Abebaw Sustained release local anesthetics for pain management: relevance and formulation approaches Frontiers in Pain Research chronic pain formulation approaches liposomal formulations lipid nanoparticles local anesthetics localized analgesia |
| title | Sustained release local anesthetics for pain management: relevance and formulation approaches |
| title_full | Sustained release local anesthetics for pain management: relevance and formulation approaches |
| title_fullStr | Sustained release local anesthetics for pain management: relevance and formulation approaches |
| title_full_unstemmed | Sustained release local anesthetics for pain management: relevance and formulation approaches |
| title_short | Sustained release local anesthetics for pain management: relevance and formulation approaches |
| title_sort | sustained release local anesthetics for pain management relevance and formulation approaches |
| topic | chronic pain formulation approaches liposomal formulations lipid nanoparticles local anesthetics localized analgesia |
| url | https://www.frontiersin.org/articles/10.3389/fpain.2024.1383461/full |
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