Lidocaine hydrochloride(LIDH) as an anesthetic is widely used in local anesthesia. Dissolving microneedles(MNs) have great application value in the field of skin anesthesia. However, the limited drug-loading of dissol...Lidocaine hydrochloride(LIDH) as an anesthetic is widely used in local anesthesia. Dissolving microneedles(MNs) have great application value in the field of skin anesthesia. However, the limited drug-loading of dissolving MNs is an existing challenge that affects clinical use. In this study, we have screened isomaltulose(ISO) as the proper matrix material for the MNs by using molecular dynamics(MD) simulation. Our findings indicate that ISO has good compatibility with LIDH, and the LIDH-loaded ISO MNs(LI-MNs) have high drug-loading capacity. The drug-loading capacity of LI-MNs could reach 80%, and it could effectively puncture the skin. In addition, the preparation method of customized LI-MNs was established based on three-dimensional(3D) printing technology. It was shown that the administration time of LI-MNs could be controlled within 3 min. Also, the LI-MNs were able to provide the local anesthetic efficacy within2 min and sustained for more than 2 h. Significantly, LI-MNs had more efficient drug efficacy compared to the topical creams and the majority of existing LIDH-loaded dissolving MNs. They even provided a longer duration of action than the injections. Overall, the LI-MNs with high drug-loading have a promising application prospect.展开更多
In cutaneous cosmetology surgery,local injection or coated anesthetics are generally used to provide analgesia at the treatment site to achieve painless operation.Due to the barrier of corneum,topical cream may cause ...In cutaneous cosmetology surgery,local injection or coated anesthetics are generally used to provide analgesia at the treatment site to achieve painless operation.Due to the barrier of corneum,topical cream may cause uncertain dosage and delayed analgesia.Local injection has problems such as pain,infection,and misoperation.Therefore,it is necessary to develop a painless and rapid administration method for local anesthesia.Here,a lidocaine/hyaluronic acid bubble microneedle patch(Lido/HA bMNP)was prepared for rapid drug delivery and efficient analgesia.The bubble structure between microneedles(MNs)and the backing layer allowed the MNs to efficiently penetrate into the skin and remove from the backing layer under shear force to rapidly complete the administration.Drugs were quickly released with the dissolution of HA within 15 s,which immediately played an analgesic effect and lasted for 1 h.Lido/HA bMNP could deliver precise doses to the skin in an extremely short time,which had the advantages of convenient operation,high biosafety,rapid onset of analgesia,and reasonable pain relief time.This patch provided an alternative way for local anesthesia and it was a promising transdermal drug delivery method for the realization of high quality and efficiency“painless medical beauty”.展开更多
基金supported by the National Key Research and Development Program of China (No.2021YFF1200800)the Sichuan Science and Technology Program (Nos.2021JDTD0001,2022YFQ0004)the Natural Science Foundation of Sichuan Province (No.2023NSFSC1629)。
文摘Lidocaine hydrochloride(LIDH) as an anesthetic is widely used in local anesthesia. Dissolving microneedles(MNs) have great application value in the field of skin anesthesia. However, the limited drug-loading of dissolving MNs is an existing challenge that affects clinical use. In this study, we have screened isomaltulose(ISO) as the proper matrix material for the MNs by using molecular dynamics(MD) simulation. Our findings indicate that ISO has good compatibility with LIDH, and the LIDH-loaded ISO MNs(LI-MNs) have high drug-loading capacity. The drug-loading capacity of LI-MNs could reach 80%, and it could effectively puncture the skin. In addition, the preparation method of customized LI-MNs was established based on three-dimensional(3D) printing technology. It was shown that the administration time of LI-MNs could be controlled within 3 min. Also, the LI-MNs were able to provide the local anesthetic efficacy within2 min and sustained for more than 2 h. Significantly, LI-MNs had more efficient drug efficacy compared to the topical creams and the majority of existing LIDH-loaded dissolving MNs. They even provided a longer duration of action than the injections. Overall, the LI-MNs with high drug-loading have a promising application prospect.
基金the National Natural Science Foundation of China(Nos.61875015 and T2125003)the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDA16021101)Beijing Natural Science Foundation(Nos.JQ20038,L212010,and L212046).
文摘In cutaneous cosmetology surgery,local injection or coated anesthetics are generally used to provide analgesia at the treatment site to achieve painless operation.Due to the barrier of corneum,topical cream may cause uncertain dosage and delayed analgesia.Local injection has problems such as pain,infection,and misoperation.Therefore,it is necessary to develop a painless and rapid administration method for local anesthesia.Here,a lidocaine/hyaluronic acid bubble microneedle patch(Lido/HA bMNP)was prepared for rapid drug delivery and efficient analgesia.The bubble structure between microneedles(MNs)and the backing layer allowed the MNs to efficiently penetrate into the skin and remove from the backing layer under shear force to rapidly complete the administration.Drugs were quickly released with the dissolution of HA within 15 s,which immediately played an analgesic effect and lasted for 1 h.Lido/HA bMNP could deliver precise doses to the skin in an extremely short time,which had the advantages of convenient operation,high biosafety,rapid onset of analgesia,and reasonable pain relief time.This patch provided an alternative way for local anesthesia and it was a promising transdermal drug delivery method for the realization of high quality and efficiency“painless medical beauty”.
