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Development of ropivacaine hydrochloride-loaded dissolving microneedles as a local anesthetic agent: A proof-of-concept.
- Source :
-
International journal of pharmaceutics [Int J Pharm] 2024 Jul 20; Vol. 660, pp. 124347. Date of Electronic Publication: 2024 Jun 15. - Publication Year :
- 2024
-
Abstract
- Ropivacaine hydrochloride (RPL) is a local anesthetic agent that has been widely used for the treatment of pain during or after surgery. However, this drug is only available in parenteral dosage form and may contribute to the infiltration of RPL into the plasma, causing some undesirable side effects. Intradermal delivery of RPL using dissolving microneedles may become a promising strategy to deliver such drugs into the skin. This research aimed to develop RPL-loaded dissolving microneedles (DMN-RPLs) as a proof of the concept of intradermal delivery of a local anesthetic. The DMN-RPLs were fabricated using either centrifugation or air-pressurized chamber methods. Several polymers, such as poly(vinyl pyrrolidone) (PVP), poly(vinyl alcohol) (PVA), and sodium hyaluronate (SH), were utilized for manufacturing the DMN-RPLs. The prepared DMN-RPLs were assessed for their thermal properties, chemical bonds, mechanical strength, insertion ability, skin-dissolution study, and drug content. Furthermore, in-skin deposition and dermatokinetic studies were also performed. The results showed that F9 (30 % w/w PVP-4 % w/w SH) and F10 (30 % w/w PVP-5 % w/w PVA) containing 5 % w/w of RPL were the most promising formulations, as shown by their needle height reduction (<10 %) and insertion depth (∼400 μm). Both formulations were also able to deliver more than 60 % of the RPL contained in the DMNs into the epidermis, dermis, and receiver compartment. This study, for the first time, has provided a proof concept to deliver RPL as a local anesthetic using DMNs and the intradermal route, aiming to minimize pain and discomfort during administration and improve the patient's experience.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2024 Elsevier B.V. All rights reserved.)
- Subjects :
- Animals
Administration, Cutaneous
Drug Liberation
Skin Absorption
Povidone chemistry
Proof of Concept Study
Solubility
Hyaluronic Acid chemistry
Hyaluronic Acid administration & dosage
Microinjections methods
Male
Rats, Sprague-Dawley
Polyvinyl Alcohol chemistry
Ropivacaine administration & dosage
Ropivacaine pharmacokinetics
Anesthetics, Local administration & dosage
Anesthetics, Local pharmacokinetics
Anesthetics, Local chemistry
Needles
Drug Delivery Systems
Skin metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3476
- Volume :
- 660
- Database :
- MEDLINE
- Journal :
- International journal of pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 38885777
- Full Text :
- https://doi.org/10.1016/j.ijpharm.2024.124347