Sustained release gel (polymer-free) of itraconazole-loaded microemulsion for oral candidiasis treatment: time-kill kinetics and cellular uptake
Drug Deliv. 2023 Dec;30(1):2234099. doi: 10.1080/10717544.2023.2234099.ABSTRACTItraconazole (ICZ) was prepared in a self-microemulsifying (SM) gel. This gel was intended for use in the oral mucosa, where low volume and flow of saliva result in limited solubility and absorption of drugs that are poorly water-soluble. The drug-loaded gel formulation (ICZ-SM) was selected as a clear solution in the ternary phase diagram to improve the solubility of ICZ. Seven ratios (S1-S7) were prepared by mixing polyoxyl 35 castor oils (P35), a medium chain with a blend of mono-, di-, and triglycerides (MCT), and water. Phase separation of ...
Source: Drug Delivery - July 14, 2023 Category: Drugs & Pharmacology Authors: Sukannika Tubtimsri Yotsanan Weerapol Source Type: research

Construction and application of microneedle-mediated photothermal therapy and immunotherapy combined anti-tumor drug delivery system
In this study, we created a microneedle drug delivery system with mercapto-modified gold nanorods and immune checkpoint blocker anti-PD-1 polypeptide. With good mechanical strength, the microneedle system can efficiently penetrate the skin and deliver drugs. When inserted into human skin, anti-PD-1 peptides and gold nanorods can be released, boosting the capacity of cytotoxic T lymphocytes to destroy tumor cells. Additionally, the elimination of the tumor is aided by the production of heat while being exposed to near-infrared light. This microneedle drug delivery system can enhance the immunological reaction and prolong th...
Source: Drug Delivery - July 13, 2023 Category: Drugs & Pharmacology Authors: Jiaqi Weng Gensuo Zheng Jiaoli Wen Jing Yang Qingliang Yang Xi Zheng Qinying Yan Source Type: research

Guanidine-modified albumin-MMAE conjugates with enhanced endocytosis ability
Drug Deliv. 2023 Dec;30(1):2219433. doi: 10.1080/10717544.2023.2219433.ABSTRACTAiming to address the insufficient endocytosis ability of traditional albumin drug conjugates, this paper reports elegant guanidine modification to improve efficacy for the first time. A series of modified albumin drug conjugates were designed and synthesized with different structures, including guanidine (GA), biguanides (BGA) and phenyl (BA), and different quantities of modifications. Then, the endocytosis ability and in vitro/vivo potency of albumin drug conjugates were systematically studied. Finally, a preferred conjugate A4 was screened, w...
Source: Drug Delivery - July 12, 2023 Category: Drugs & Pharmacology Authors: Ce Yi Fei Xie Xin Xu Dian Xiao Xinbo Zhou Maosheng Cheng Source Type: research

A click chemistry-based, free radical-initiated delivery system for the capture and release of payloads
Drug Deliv. 2023 Dec;30(1):2232952. doi: 10.1080/10717544.2023.2232952.ABSTRACTClick chemistries are efficient and selective reactions that have been leveraged for multi-stage drug delivery. A multi-stage system allows independent delivery of targeting molecules and drug payloads, but targeting first-phase materials specifically to disease sites remains a challenge. Stimuli-responsive systems are an emerging strategy where common pathophysiological triggers are used to target payloads. Oxidative stress is widely implicated in disease, and we have previously demonstrated that reactive oxygen species (ROS) can crosslink and ...
Source: Drug Delivery - July 12, 2023 Category: Drugs & Pharmacology Authors: Emily T DiMartini Kelly Kyker-Snowman David I Shreiber Source Type: research

Guanidine-modified albumin-MMAE conjugates with enhanced endocytosis ability
Drug Deliv. 2023 Dec;30(1):2219433. doi: 10.1080/10717544.2023.2219433.ABSTRACTAiming to address the insufficient endocytosis ability of traditional albumin drug conjugates, this paper reports elegant guanidine modification to improve efficacy for the first time. A series of modified albumin drug conjugates were designed and synthesized with different structures, including guanidine (GA), biguanides (BGA) and phenyl (BA), and different quantities of modifications. Then, the endocytosis ability and in vitro/vivo potency of albumin drug conjugates were systematically studied. Finally, a preferred conjugate A4 was screened, w...
Source: Drug Delivery - July 12, 2023 Category: Drugs & Pharmacology Authors: Ce Yi Fei Xie Xin Xu Dian Xiao Xinbo Zhou Maosheng Cheng Source Type: research

A click chemistry-based, free radical-initiated delivery system for the capture and release of payloads
Drug Deliv. 2023 Dec;30(1):2232952. doi: 10.1080/10717544.2023.2232952.ABSTRACTClick chemistries are efficient and selective reactions that have been leveraged for multi-stage drug delivery. A multi-stage system allows independent delivery of targeting molecules and drug payloads, but targeting first-phase materials specifically to disease sites remains a challenge. Stimuli-responsive systems are an emerging strategy where common pathophysiological triggers are used to target payloads. Oxidative stress is widely implicated in disease, and we have previously demonstrated that reactive oxygen species (ROS) can crosslink and ...
Source: Drug Delivery - July 12, 2023 Category: Drugs & Pharmacology Authors: Emily T DiMartini Kelly Kyker-Snowman David I Shreiber Source Type: research

Triptorelin nanoparticle-loaded microneedles for use in assisted reproductive technology
We report silk fibroin (SF)-based microneedles (MNs) for transdermal delivery of triptorelin-loaded nanoparticles (NPs) to improve bioavailability and achieve safe and efficacious self-administration of triptorelin. Triptorelin was mixed into an aqueous solution of SF with shear force to prepare NPs to control the release and avoid the degradation of triptorelin by enzymes in the skin. Two-step pouring and centrifugation were employed to prepare nanoparticles-encapsulated polymeric microneedles (NPs-MNs). An increased β-sheet content in the conformation ensured that NPs-MNs had good mechanical properties to pierce the str...
Source: Drug Delivery - June 30, 2023 Category: Drugs & Pharmacology Authors: Xiaoyan Lu Yiying Sun Meishan Han Daoyuan Chen Xiaoyan He Siqi Wang Kaoxiang Sun Source Type: research