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Quality evaluation of lidocaine hydrochloride rapid onset local anesthesia preparation based on microneedles technology
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Hao-hui ZHAN, Ying-cong HUANG, Feng-sen MA*
Acta Pharmaceutica Sinica | 2018, 53(8) : 1371 - 1376
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Acta Pharmaceutica Sinica | 2018, 53(8): 1371-1376
ORIGINAL ARTICLES
Quality evaluation of lidocaine hydrochloride rapid onset local anesthesia preparation based on microneedles technology
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Hao-hui ZHAN, Ying-cong HUANG, Feng-sen MA*
Affiliations
  • College of Pharmacy, Zhejiang University of Technology, Hangzhou 310014, China
Published: 2018-08-12 doi: 10.16438/j.0513-4870.2018-0278
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Microneedles is an efficient, safe and novel transdermal drug delivery technology that has attracted much attention in recent decades. Microneedles could break through the skin's stratum corneum barrier and have an especially significant effect on the transdermal delivery of water-soluble small molecules and biological macromolecules. In this paper, a rapid onset local anesthetic preparation of lidocaine hydrochloride was prepared based on dissolving microneedles, and related quality evaluations were carried out. The key quality indicators of prepared lidocaine hydrochloride dissolving microneedles such as drug loading amount, appearance morphology, mechanical properties, skin penetration performance, in vitro dissolution performance and local anesthetic efficacy were investigated with HPLC, SEM, texture analyzer, organic staining, histological section, in vitro dissolution test and pharmacodynamics experiments respectively. The drug loading of the dissolving microneedles array reached 68.19 ±1.55 mg, and the needle tip contained 3.57 ±0.21 mg. The microneedles has good needle shape and sufficient mechanical strength to penetrate into the skin, which is a prerequisite for the successful administration of the preparation. The in vitro dissolution time was 28.28 ±1.12 s. When applied to guinea pig back acupuncture model which was modified by guinea pig intradermal papules model, although the efficacy maintenance time was shorter than that of compound lidocaine cream, dissolving microneedles can be activated within 1 min, which was much faster than compound lidocaine cream. It is possible to increase the duration of drug efficacy by increasing the density of microneedles and preparing microneedles for sustained and controlled release in future studies. Lidocaine hydrochloride dissolving microneedles and its evaluation methods for local anesthesia were established systematically here for the first time. The rapid effect of anesthesia with lidocaine hydrochloride dissolving microneedles on the skin was worthy of further investigation.

lidocaine hydrochloride  /  transdermal administration  /  local anesthesia  /  pharmacodynamics
Hao-hui ZHAN, Ying-cong HUANG, Feng-sen MA. Quality evaluation of lidocaine hydrochloride rapid onset local anesthesia preparation based on microneedles technology[J]. Acta Pharmaceutica Sinica, 2018 , 53 (8) : 1371 -1376 . DOI: 10.16438/j.0513-4870.2018-0278
Year 2018 volume 53 Issue 8
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doi: 10.16438/j.0513-4870.2018-0278
  • Receive Date:2018-03-27
  • Online Date:2026-01-15
  • Published:2018-08-12
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  • Received:2018-03-27
  • Revised:2018-05-09
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    College of Pharmacy, Zhejiang University of Technology, Hangzhou 310014, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
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Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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