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Journal Drug Deliv

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Endostatin in fibrosis and as a potential candidate of anti-fibrotic therapy.

Zequn Zhang, Xi Liu, Zhaolong Shen, Jun Quan, Changwei Lin, Xiaorong Li, Gui Hu,

Fibrotic diseases pose significant clinical challenges due to their broadness and complexity. Thus, a better understanding of fibrogenesis and the development of more effective treatments is imperative. Recent evidence suggests a significant antifibrotic potential of an endogenous glycoprotein, endostatin. While endostatin has been widely studied for its role as an ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):2051-2061]

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Formulation, characterization, optimization, and in-vivo performance of febuxostat self-nano-emulsifying system loaded sublingual films.

Basant A Habib, Amina S Abd El-Samiae, Boushra M El-Houssieny, Randa Tag,

Febuxostat (FXS) is a potent antigout drug with poor water solubility and relative high first-pass effect leading to moderate oral bioavailability (<49%). This study aimed to increase FXS solubility and bioavailability by optimizing sublingual fast-dissolving films (SFs) containing a selected FXS self-nano-emulsifying system (s-SNES) previously prepared by our team. The ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1321-1333]

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Drug distribution along the cochlea is strongly enhanced by low-frequency round window micro vibrations.

Samuel M Flaherty, Ian J Russell, Andrei N Lukashkin,

The cochlea's inaccessibility and complex nature provide significant challenges to delivering drugs and other agents uniformly, safely and efficiently, along the entire cochlear spiral. Large drug concentration gradients are formed along the cochlea when drugs are administered to the middle ear. This undermines the major goal of attaining therapeutic drug ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1312-1320]

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Enhancing the in vitro and in vivo activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules.

Nabila A El-Sheridy, Riham M El-Moslemany, Alyaa A Ramadan, Maged W Helmy, Labiba K El-Khordagui,

Itraconazole (ITC), a well-tolerated antifungal drug, exerts multiple anticancer effects which justified its preclinical and clinical investigation as potential anti-cancer agent with reduced side effects. Enhancement of ITC anti-cancer efficacy would bring valuable benefits to patients. We propose herein lipid nanocapsules (LNCs) modified with a subtherapeutic dose of miltefosine (MFS) ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):906-919]

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Controllable release of pirfenidone by polyvinyl alcohol film embedded soft contact lenses in vitro and in vivo.

Caiqing Wu, Ping Wai Or, Jones Iok Tong Chong, Isuru K K Pathirage Don, Ching Hymn Christopher Lee, Kaili Wu, Minbin Yu, David C C Lam, Yangfan Yang,

To increase the amount of pirfenidone (PFD) loaded in polyvinyl alcohol (PVA) film embedded soft contact lens (SCL), and evaluate its function of sustaining delivery of drug <i>in vitro</i> and <i>in vivo</i>. Drug loading efficiency within PVA film and SCLs, drug release from SCLs <i>in vitro</i>, and the effects of parameters of SCLs ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):634-641]

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Development and in vivo evaluation of intranasal formulations of parathyroid hormone (1-34).

Dan Wang, Yimeng Du, Wenpeng Zhang, Xiaolu Han, Hui Zhang, Zengming Wang, Nan Liu, Meng Li, Xiang Gao, Xiaomei Zhuang, Jing Gao, Aiping Zheng,

For efficient intranasal transport of parathyroid hormone (1-34) [PTH(1-34)], there is a great medical need to investigate permeation enhancers for intranasal formulations. In this study, the development of PTH(1-34) intranasal formulations was conducted. Based on conformation and chemical stability studies, the most preferable aqueous environment was determined to be 0.008 M ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):487-498]

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Gelatin hydrogel/contact lens composites as rutin delivery systems for promoting corneal wound healing.

Lianghui Zhao, Xia Qi, Tao Cai, Zheng Fan, Hongwei Wang, Xianli Du,

Corneal wound healing is a highly regulated biological process that is of importance for reducing the risk of blinding corneal infections and inflammations. Traditional eye drop was the main approach for promoting corneal wound healing. However, its low bioavailability required a high therapeutic concentration, which can lead to ocular or ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1951-1961]

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Transdermal delivery of triptolide-phospholipid complex to treat rheumatoid arthritis.

Xin-Yi Liu, Wen-Jun Pei, Ye-Zhen Wu, Fang-Li Ren, Si-Yu Yang, Xiu Wang,

The aim of this study was to develop and evaluate a triptolide phospholipid complex (TPCX) for the treatment of rheumatoid arthritis (RA) by transdermal delivery. TPCX was prepared and characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR) analysis, transmission electron microscope (TEM), and scanning electron microscope (SEM). The ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):2127-2136]

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Targeting delivery and minimizing epidermal diffusion of tranexamic acid by hyaluronic acid-coated liposome nanogels for topical hyperpigmentation treatment.

Ying Liu, Yue Han, Tingting Zhu, Xianglei Wu, Wenxin Yu, Jiafang Zhu, Ying Shang, Xiaoxi Lin, Tianlan Zhao,

Hyperpigmentation is a common complaint and distressing problem in dermatology, and tranexamic acid (TA) is an effective treatment agent but limited by the delivery to melanocytes in the epidermis. Herein, a novel TA naogels (named HA/TA-LP), combining the advantages of liposomes and hyaluronic acid (HA), are prepared and assessed for ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):2100-2107]

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Study on mechanism of low bioavailability of black tea theaflavins by using Caco-2 cell monolayer.

Fengfeng Qu, Zeyi Ai, Shuyuan Liu, Haojie Zhang, Yuqiong Chen, Yaomin Wang, Dejiang Ni,

This study aimed to clarify the bioavailability mechanism of theaflavins by using the Caco-2 monolayer <i>in vitro</i> model. Prior to the transport of theaflavin (TF), theaflavin-3-gallate (TF3G), theaflavin-3'-gallate (TF3'G), and theaflavin-3, 3'-digallate (TFDG), we found the cytotoxicity of theaflavins was in the order of TF3'G > TFDG > TF3G > TF, suggesting the galloyl moiety enhances ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1737-1747]

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UTMD promoted local delivery of miR-34a-mimic for ovarian cancer therapy.

Yue Li, Meng Du, Jinghui Fang, Jia Zhou, Zhiyi Chen,

MicroRNA-mediated gene therapy is emerging as a promising method for the treatment of ovarian cancer, but the development of miRNA mimic delivery vectors is still in its infancy, where the safety and efficacy of miR-34a-mimic remain unknown. Ultrasound-targeted microbubble destruction (UTMD) can be an effective and minimally invasive tool for ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1616-1625]

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Synergic fabrication of pembrolizumab loaded doxorubicin incorporating microbubbles delivery for ultrasound contrast agents mediated anti-proliferation and apoptosis.

Huilin Liu, Xing Li, Zihe Chen, Lianjie Bai, Ying Wang, Weiyang Lv,

This study evaluated pembrolizumab-conjugated, doxorubicin (DOX)-loaded microbubbles (PDMs) in combination with ultrasound (US) as molecular imaging agents for early diagnosis of B cell lymphomas, and as a targeted drug delivery system. Pembrolizumab, a monoclonal CD20 antibody, was attached to the surfaces of DOX-loaded microbubbles. PDM binding to B cell lymphoma ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1466-1477]

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Development of a human antibody fragment directed against the alpha folate receptor as a promising molecule for targeted application.

Nattihda Parakasikron, Chatchai Chaotham, Pithi Chanvorachote, Chanida Vinayanuwattikun, Visarut Buranasudja, Pornchanok Taweecheep, Kannika Khantasup,

Alpha folate receptor (FRα) is currently under investigation as a target for the treatment of patients with non-small-cell lung cancer (NSCLC), since it is highly expressed in tumor cells but is largely absent in normal tissue. In this study, a novel human variable domain of a heavy-chain (VH) antibody fragment ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1443-1454]

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Engineering of injectable hydrogels associate with Adipose-Derived stem cells delivery for anti-cardiac hypertrophy agents.

Guangyu Long, Quanhe Wang, Shaolin Li, Junzhong Tao, Boyan Li, Xiangxiang Zhang, Xi Zhao,

Adipose-derived stem cells (ADSCs) treatment offers support to new methods of transporting baseline cell protein endothelial cells in alginate (A)/silk sericin (SS) lamellar-coated antioxidant system ([email protected]) to promote acute myocardial infarction. In the synthesized frames of ASS, the ratio of fixity modules, pores, the absorption and inflammation was detected at ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1334-1341]

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Bleomycin administered by laser-assisted drug delivery or intradermal needle-injection results in distinct biodistribution patterns in skin: in vivo investigations with mass spectrometry imaging.

Kristoffer Hendel, Anders C N Hansen, Liora Bik, Charlotte Bagger, Martijn B A van Doorn, Christian Janfelt, Uffe H Olesen, Merete Haedersdal, Catharina M Lerche,

Bleomycin (BLM) is being repositioned in dermato-oncology for intralesional and intra-tumoural use. Although conventionally administered by local needle injections (NIs), ablative fractional lasers (AFLs) can facilitate topical BLM delivery. Adding local electroporation (EP) can augment intracellular uptake in the target tissue. Here, we characterize and compare BLM biodistribution patterns, cutaneous ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1141-1149]

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Oral gel loaded with penciclovir-lavender oil nanoemulsion to enhance bioavailability and alleviate pain associated with herpes labialis.

Khaled M Hosny, Amal M Sindi, Hala M Alkhalidi, Mallesh Kurakula, Nabil K Alruwaili, Nabil A Alhakamy, Walaa A Abualsunun, Rana B Bakhaidar, Rahaf H Bahmdan, Waleed Y Rizg, Sarah A Ali, Wesam H Abdulaal, Majed S Nassar, Mohammed S Alsuabeyl, Adel F Alghaith, Sultan Alshehri,

Herpes labialis, caused by herpes simplex virus type 1, is usually characterized by painful skin or mucosal lesions. Penciclovir (PV) tablets are found to be effective against herpes labialis but suffer from poor oral bioavailability. This study aimed to combine the benefits of PV and lavender oil (LO), which exhibits ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1043-1054]

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Targeted nano-delivery strategies for facilitating thrombolysis treatment in ischemic stroke.

Hongyin Ma, Zhenmin Jiang, Jiayun Xu, Junqiu Liu, Zhen-Ni Guo,

Ischemic stroke is one of the major causes of severe disability and death worldwide. It is mainly caused by a sudden reduction in cerebral blood flow due to obstruction of the supplying vessel by thrombi and subsequent initiation of a complex cascade of pathophysiological changes, which ultimately lead to brain ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):357-371]

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Β-Cyclodextrin-graft-poly(amidoamine) dendrons as the nitric oxide deliver system for the chronic rhinosinusitis therapy.

Tao Liu, Guowei Li, Xidong Wu, Shaohua Chen, Siyi Zhang, Hong Han, Hongbin Zhang, Xiaoning Luo, Xiang Cai, Dong Ma,

Chronic rhinosinusitis (CRS) is a rather prevalent condition with a chronic inflammatory process, which is hard to cure. Herein, a new antibacterial drug, nitric oxide (NO), was used for the attempt on CRS therapy. To achieve this, a star copolymer (β-CD-PAMAM) consisting of the β-cyclodextrin (β-CD) core and seven PAMAM-G3 ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):306-318]

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Management of recurrent aphthous ulcers exploiting polymer-based Muco-adhesive sponges: in-vitro and in-vivo evaluation.

Muhammed Ossama, Caroline Lamie, Mohamed Tarek, Hebatallah A Wagdy, Dalia A Attia, Mohamed M Elmazar,

Recurrent aphthous ulcer (RAU) is a well-known painful, inflammatory disease with uncertain etiology for which local symptomatic therapy is only available. The aim of this study was to formulate and characterize muco-adhesive sponges containing a mixture of tenoxicam and miconazole nitrate to manage pain, inflammation and avoid candida infection that ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):87-99]

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Experimental anti-tumor effect of emodin in suspension - in situ hydrogels formed with self-assembling peptide.

Weipeng Wei, Jianhua Tang, Lei Hu, Yujie Feng, Hongfang Li, Chengchen Yin, Fushan Tang,

Lung cancer is a major cause of cancer-related deaths worldwide. Stimulus-sensitive hydrogels, which can be formed by responding to stimuli in the cancer microenvironment, have been widely studied as controlled-release carriers for hydrophobic anticancer drugs. In this study, self-assembling peptide RADA16-I was used to encapsulate the hydrophobic drug emodin (EM) ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1810-1821]

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A bivalent cyclic RGD-siRNA conjugate enhances the antitumor effect of apatinib via co-inhibiting VEGFR2 in non-small cell lung cancer xenografts.

Lumin Liao, Bohong Cen, Guoxian Li, Yuanyi Wei, Zhen Wang, Wen Huang, Shuai He, Yawei Yuan, Aimin Ji,

The vascular endothelial growth factor receptor 2 (VEGFR2) is considered to be a pivotal target for anti-tumor therapy against angiogenesis of non-small cell lung cancer (NSCLC). However, effective and low-toxicity targeted therapies to inhibit VEGFR2 are still lacking. Here, biRGD-siVEGFR2 conjugate comprising murine VEGFR2 siRNA and [cyclo(Arg-Gly-Asp-D-Phe-Lys)-Ahx]<sub>2</sub>-Glu-PEG-MAL (biRGD) peptide which ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):1432-1442]

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Drug delivery of amoxicillin molecule as a suggested treatment for covid-19 implementing functionalized mesoporous SBA-15 with aminopropyl groups.

Haneen F Alazzawi, Issam K Salih, Talib M Albayati,

SARS-CoV-2 is a novel coronavirus that was isolated and identified for the first time in Wuhan, China in 2019. Nowadays, it is a worldwide danger and the WHO named it a pandemic. In this investigation, a functionalization post-synthesis method was used to assess the ability of an adapted SBA-15 surface ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):856-864]

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Inhalation delivery dramatically improves the efficacy of topotecan for the treatment of local and distant lung cancer.

Philip J Kuehl, Christin M Yingling, Devon Dubose, Michael Burke, David A Revelli, Wenshu Chen, Wendy W Dye, Steven A Belinsky, Mathewos Tessema,

Topotecan is potent anti-cancer drug approved for various malignancies but hematopoietic toxicities undermine its wider application and use of its most effective dose. This study aims to improve these limitations through inhalation-delivery. The pharmacokinetics, efficacy, and toxicity of 2-5 times lower inhalation doses of topotecan dry-powder were compared with the ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):767-775]

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Charge-reversal nanomedicine based on black phosphorus for the development of A Novel photothermal therapy of oral cancer.

Zimu Li, Qingyun Liu, Yi Zhang, Yao Yang, Xiaomin Zhou, Wei Peng, Zhigang Liang, Xiaowei Zeng, Qiuxu Wang, Nansha Gao,

Driven by the lifestyle habits of modern people, such as excessive smoking, drinking, and chewing betel nut and other cancer-causing foods, the incidence of oral cancer has increased sharply and has a trend of becoming younger. Given the current mainstream treatment means of surgical resection will cause serious damage to ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):700-708]

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Skin-specific knockdown of hyaluronan in mice by an optimized topical 4-methylumbelliferone formulation.

Emily H Steen, Walker D Short, Hui Li, Umang M Parikh, Alexander Blum, Natalie Templeman, Nadine Nagy, Paul L Bollyky, Sundeep G Keswani, Swathi Balaji,

Hyaluronan (HA) is abundant in the skin; while HA can be synthesized by the synthases (HAS1-3), HAS2 is the leading contributor. Dysregulation and accumulation of HA is implicated in the pathogenesis of diseases such as keloid scarring, lymphedema and metastatic melanoma. To understand how HA synthesis contributes to skin physiology, ... Read more >>

Drug Deliv (Drug delivery)
[2021, 28(1):422-432]

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