Design and evaluation of pH-responsive hydrogel for oral delivery of amifostine and study on its radioprotective effects

Lin, Xiaona; Miao, Longfei; Wang, Xinxin; Tian, Hongqi

doi:10.1016/j.colsurfb.2020.111200

Cited by 25 publications

(18 citation statements)

References 27 publications

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“…Lin et al prepared amifostine‐loaded hydrogel by grafting polycaprolactone onto a methacrylic acid copolymer. In vitro drug release studies confirmed that this hydrogel system released a negligible amount of drug in simulated gastric‐fluid (SGF), and a burst release was observed in simulated small intestinal fluid (SIF) 161 . Apart from developing matrix‐type systems, a drug reservoir coated with gastro‐resistant polymer offers convenience and a better release profile.…”

Section: Applications Of Polyelectrolytes In Drug Deliverymentioning

confidence: 74%

“…In vitro drug release studies confirmed that this hydrogel system released a negligible amount of drug in simulated gastric-fluid (SGF), and a burst release was observed in simulated small intestinal fluid (SIF). 161 Apart from developing matrix-type systems, a drug reservoir coated with gastro-resistant polymer offers convenience and a better release profile. Eudragit ® L 100 is a commonly used polymer for making enteric-coated/delayed-release pellets/ tablets for rendering acid-labile drugs gastro-resistant.…”

Section: Small Intestinal Drug Deliverymentioning

confidence: 99%

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pH‐responsive polymers for drug delivery: Trends and opportunities

Singh,

Nayak

2023

Journal of Polymer Science

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Polymer science has applications in biomedical engineering, prosthetics, surgical implants, and prospective pharmaceutical excipients for drug delivery. “Intelligent or Smart Polymers” are created for drug targeting either by derivatization of natural polymers or controlled radical polymerization of electrolytes. Their mode of action is governed by the environmental stimuli viz. temperature, pH, ionic concentration, magnetism, and so on. pH‐responsive polymers, because of their self‐assembling behavior, alter their solubility, conformation, surface activity, and hydrophilicity when exposed to a specific pH. The physiological pH varies from acidic nuclei to alkaline cytoplasm and highly acidic gastric juice to slightly alkaline plasma; thus, various polymers are under study for delivering small molecules, genes, peptides, enzymes, growth factors, and antibodies. The non‐invasive drug delivery routes like oral, ocular, nasal, pulmonary, transdermal, and rectal routes can be explored for targeting recombinant proteins, monoclonal antibodies, and small molecules with particular emphasis on the individual's physiological and pathological state. Further, these polymers can be designed into various architectures like dendrimers, liposomes, micelles, and metallic nanoparticles that can serve as drug reservoirs for sustaining drug release. The challenges in this field are the selection of biocompatible polymers with ease of synthesis and scale‐up, ensuring effective drug‐loading, and stability aspects, producing robust pharmacological data, and timely regulatory approvals. This review exclusively explores the physicochemical characteristics of pH‐responsive polymers, their categorization, various architectural entities, recent studies and patents, and their emerging applications concerning specific diseases.

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Section: Applications Of Polyelectrolytes In Drug Deliverymentioning

confidence: 74%

Section: Small Intestinal Drug Deliverymentioning

confidence: 99%

pH‐responsive polymers for drug delivery: Trends and opportunities

Singh,

Nayak

2023

Journal of Polymer Science

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“…To date, the potential radiation hazard has become a serious public health challenge due to the rapid development and wide application of the nuclear industry [ 26 ]. Especially radioprotectors should be safe, effective, and easy-to-administer because they should be given to military personnel and first responders prior to entering a known radiation area [ 27 ].…”

Section: Discussionmentioning

confidence: 99%

Preclinical Evaluation of Safety, Pharmacokinetics, Efficacy, and Mechanism of Radioprotective Agent HL‐003

Liu

Miao

Tian

2021

Oxidative Medicine and Cellular Longevity

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Amifostine is a radioprotector with high efficacy but poor safety, short half-life, no oral formulation, and poor compliance, which limits its application. With the increasing risk of exposure to radiation, the development of new radioprotective agents is critical. We previously synthesized a new amifostine derivative, the small molecule compound HL-003. In this study, we focused on evaluating the radioprotective properties of HL-003. Using the in vitro 2,2-diphenyl-1-picrylhydrazyl assay, we initially confirmed HL-003 as a strong antioxidant and demonstrated that its free radical scavenging activity was stronger than that of amifostine. Then, we performed an acute toxicity test, a 28-day toxicity test, a 30-day survival rate test, and a pharmacokinetic study, all of which provided aggregate evidence that HL-003 functioned as a small molecule radioprotector with high efficacy, a favorable safety profile, a long half-life, and oral administration. The intestinal radioprotective mechanism of HL-003 was explored in male C57 mice after abdominal irradiation by analyzing intestinal tissue samples with hematoxylin-eosin staining, immunohistochemistry, TUNEL staining, and immunofluorescence detection. The results showed that HL-003 protected intestinal DNA from radiation damage and suppressed the expression of phosphorylated histone H2AX, phosphorylated p53, and the apoptosis-related proteins caspase-8 and caspase-9, which contributed to maintaining the normal morphology of the small intestine and provided insights into the mechanism of radioprotection. Thus, HL-003 is a small molecule radioprotector with a potential application in radiation medicine.

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“…Xiaona Lin et al connected poly(caprolactone) (PCL) to methacrylic acid copolymer (MAC-g-PCL) to prepare hydrogels. 82 As a hydrophobic biomaterial, PCL was grafted to MAC to improve its stability and hydrogel performance. Compared with nanoparticles, hydrogels have faster drug loading speed and no solvent.…”

Section: Other New Drug Delivery Systemsmentioning

confidence: 99%

Advances of Amifostine in Radiation Protection: Administration and Delivery

Ji,

Cui,

Zhou

et al. 2023

Mol. Pharmaceutics

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Amifostine (AMF, also known as WR-2721) is the only approved broad-spectrum small-molecule radiation protection agent that can combat hematopoietic damage caused by ionizing radiation and is used as an antitumor adjuvant and cell protector in cancer chemotherapy and radiotherapy. Amifostine is usually injected intravenously before chemotherapy or radiotherapy and has been used in the treatment of head and neck cancer. However, the inconvenient intravenous administration and its toxic side effects such as hypotension have severely limited its further application in clinic. In order to reduce the toxic and side effects, scientists are trying to develop a variety of drug administration methods and are devoted to developing a wide application of amifostine in radiation protection. This paper reviews the research progress of amifostine for radiation protection in recent years, discusses its mechanism of action, clinical application, and other aspects, with focus on summarizing the most widely studied amifostine injection administration and drug delivery systems, and explored the correlation between various administrations and drug efficacies.

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Design and evaluation of pH-responsive hydrogel for oral delivery of amifostine and study on its radioprotective effects

Cited by 25 publications

References 27 publications

pH‐responsive polymers for drug delivery: Trends and opportunities

pH‐responsive polymers for drug delivery: Trends and opportunities

Preclinical Evaluation of Safety, Pharmacokinetics, Efficacy, and Mechanism of Radioprotective Agent HL‐003

Advances of Amifostine in Radiation Protection: Administration and Delivery

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