Celebrating the 30th Anniversary of the Department of Environmental Science and Engineering, Fudan University.
Fang Mingliang M, Zhang Liwu L, Wang Lin L, Chen Jianmin J
Shanghai Fudan-Zhangjiang · TOP2A · 小分子
doxorubicin hydrochloride 是一种小分子,由Shanghai Fudan-Zhangjiang研发。该药已获批,用于治疗相关适应症,给药途径:Injectable (Others)、Intravenous (IV)。
| 商品名 | Libod, Libaoduo |
| 公司 | Shanghai Fudan-Zhangjiang |
| 药物类别 | 小分子 |
| 分子靶点 | TOP2A |
| 给药途径 | Injectable (Others), Intravenous (IV) |
| 状态 | Approved |
doxorubicin hydrochloride 作用于 1 个分子靶点:
| TOP2A | DNA topoisomerase II alpha (TOP2alpha, TOPIIA) |
doxorubicin hydrochloride 针对 4 个适应症,涉及 1 个治疗领域。
| 治疗领域 | 疾病/病症 | 分期 |
|---|---|---|
| Neoplasms benign, malignant and unspecified (incl cysts and polyps) | Breast cancer | ✓ Approved |
| Neoplasms benign, malignant and unspecified (incl cysts and polyps) | Kaposi's sarcoma | ✓ Approved |
| Neoplasms benign, malignant and unspecified (incl cysts and polyps) | Ovarian cancer | ✓ Approved |
| Neoplasms benign, malignant and unspecified (incl cysts and polyps) | Plasma cell myeloma | ✓ Approved |
Fang Mingliang M, Zhang Liwu L, Wang Lin L, Chen Jianmin J
Lakatos Botond B, Burzynski Emily E, Bou Chahine Janah J, Bennacer Leyla L et al.
Human herpesvirus 8 (HHV-8) is associated with Kaposi sarcoma (KS), multicentric Castleman disease (MCD), and primary effusion lymphoma (PEL), important causes of morbidity among people living with HIV. Data on these diseases remain limited from Central and Eastern Europe compared with Western Europe. We conducted a multicentre cross-sectional survey, using an online questionnaire distributed to HIV physicians within the Euroguidelines in Central and Eastern Europe Network Group, comprising epidemiology, diagnostic capacity, and management of HHV-8-related diseases. Twenty-six HIV treatment centres from 22 countries participated, providing care for 36,845 people living with HIV. A total of 55 cases of KS (1.49 per 1000 PLWH) were reported, of which 35 (63.6%) had visceral involvement. MCD and PEL were uncommon, with 7 and 4 cases, respectively. Diagnostic capacity varied between centres: computed tomography was available in 80.8%, bronchoscopy in 30.8%, and gastroscopy in 23.1%. Antiretroviral therapy alone was the most common first-line treatment for limited KS, while pegylated liposomal doxorubicin was accessible as first-line and/or second-line treatment in 46.2% of centres. HHV-8-related diseases remain uncommon but clinically relevant complications of HIV infection in Central and Eastern Europe. Regional variability in diagnostic resources and treatment availability highlights the need for strengthened referral pathways and guideline-adherent care.
Cheng Xi X, Li Mengyuan M, Yan Shen S, Zhang Shengyu S et al.
Objectives: Aqueous liposomal suspensions suffer from inherent physical and chemical instability, motivating the development of solid powder formulations. Spray-freeze-drying is a promising solidification technique; however, systematic investigations that isolate the impact of individual unit operations-atomization, freezing, and drying-on liposomal stability remain scarce. This study aimed to elucidate the stage-specific effects of each unit operation on the critical quality attributes of liposomal powders. Methods: Ovalbumin-loaded liposomes (O@L) prepared from DSPC, HSPC, or DPPC were processed using a self-developed microfluidic jet spray freezing tower coupled to a freeze dryer, with trehalose or mannitol as cryoprotectants. The effects of phospholipid composition, freezing temperature (-30 °C, -50 °C, and -70 °C), and freeze-drying cycle were assessed through the z-average, zeta potential, and encapsulation efficiency (EE) of the reconstituted liposomes, as well as the morphology, crystallinity, residual moisture, and hygroscopicity of the resulting powders. Results: Atomization induced protein leakage from the trehalose formulations, whereas mannitol better preserved EE. During freezing, trehalose provided superior cryoprotection, as mannitol partially crystallized and failed to uniformly coat the vesicles. After drying, however, vesicles frozen at -70 °C exhibited fusion attributable to non-uniform cryoprotectant distribution; a moderate freezing temperature (-50 °C) combined with a stepwise primary drying program proved optimal. Trehalose-based powders displayed higher residual moisture and irreversible crystallization above ~60% RH, whereas crystalline mannitol ensured low, reversible hygroscopicity. Conclusions: The optimal condition for a single unit operation does not guarantee the best overall outcome; rational spray-freeze-drying process design requires balancing stage-specific effects.
Ciuca Maria D MD, Racovita Radu C RC
Use of antidepressant medication has increased substantially nowadays. Investigations of their photostability in aqueous environment are therefore needed both for shelf life assessment of liquid pharmaceutical formulations and for development of wastewater remediation technologies. In this work, the comparative kinetics of photodegradation of five tricyclic antidepressants (TCAs) in aqueous solution was studied under direct photolysis using UVA, UVB, and UVC sources, respectively. A gas chromatography-mass spectrometry (GC-MS) method was developed and validated intra-laboratory for accurate quantification of the five TCAs (amitriptyline hydrochloride AMI, doxepin hydrochloride DOX, imipramine hydrochloride IMI, clomipramine hydrochloride CLO, trimipramine maleate TRI) in the course of photodegradation. UVC photolysis yielded the highest rates of photodegradation, followed by UVB and then UVA. The molecular structure and UV absorption characteristics of individual TCAs were shown to influence photodegradation rates as well. Specifically, heteroatoms (N, O, Cl) present in the molecule and redshifted UV absorption bands increased photosensitivity typically in the order: AMI < IMI < TRI < CLO < DOX. The effect that some mono- and polycarboxylic acids dissolved in the aqueous solutions had on TCA photodegradation kinetics under UVC was also investigated and, for most TCAs, rates were faster and durations required for their complete photodegradation decreased generally in the order: citric > oxalic > maleic > benzoic acid. Furthermore, citric acid was reused for a second round of TCA photodegradation and showed rate enhancement effects very close to those exhibited in the first round.
Crețeanu Andreea A, Lungu Claudiu N CN, Gratiela Popa Eliza E, Tartau Liliana Mititelu LM et al.
Oncology and cardiology use paclitaxel, a powerful cell-division inhibitor. Paclitaxel-eluting coated metal stents in oncology prevent tumor growth by modulating proliferation, apoptosis, and angiogenesis. Paclitaxel-eluting stents reduce in-stent restenosis and maintain arterial patency in cardiology. Paclitaxel encapsulated in liposomes improves targeted administration, pharmacokinetics, and therapeutic efficacy. Liposome-loaded paclitaxel has a stronger anti-tumor effect than standard formulations. Paclitaxel plus sirolimus in a stent may synergistically prevent restenosis and inhibit tumors. Liposomal formulations with supplemental medications offer promising prospects for improving therapeutic accuracy and efficacy. Liposomal paclitaxel enhances targeted drug delivery, which may improve cancer treatment and cardiovascular treatments such as drug-eluting stents and drug-coated balloons in interventional radiology. Advanced delivery technologies have changed paclitaxel drug delivery methods for therapeutic use by overcoming its low solubility and systemic toxicity. Nanocrystals and liposomes enable high drug loading and precise targeted delivery, and, by eliminating toxic solvents such as Cremophor EL, they improve the safety and efficacy of cancer therapy.
Avdeev Vadim V VV, Vladimirsky Mikhail A MA, Eliseev Platon I PI, Samoilova Anastasia G AG et al.
The global spread of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB) demands fundamentally new approaches combining diagnostic speed and therapeutic efficacy. Within the strategy of personalised medicine, the lytic mycobacteriophage D29 represents a promising tool for both phenotypic drug susceptibility testing and the targeted delivery of therapeutic agents to the infection site. We developed a two-component platform based on D29: (1) a diagnostic test system combining a rapid anti-mycobacterial susceptibility testing (AMST) module, which detects phage D29 replication in drug-resistant isolates via multiplex real-time PCR; and (2) a liposomal therapeutic formulation. Therapeutic efficacy was evaluated in C57BL/6 mice (n = 55) with experimental pulmonary tuberculosis receiving liposomal D29 either aerosolised (inhalation chamber) or intranasally. Bacterial burden (CFU/lung) was assessed at days 3 and 14 post-therapy. Pharmacokinetics were studied in 90 mice using the double-layer agar method. The diagnostic test showed an average sensitivity and specificity of 90.0% and 96.3% across nine drugs, with results available within five days. The lyophilised components and phage remained stable for 12 months. Aerosol therapy demonstrated a trend towards a higher efficacy compared to intranasal administration: the median CFU/lung at day 3 was 107 (i.e., one hundred and seven) vs. 23,500 (control 65,000); 60% of aerosol-treated animals achieved ≤200 CFU/lung (not statistically significant, p = 0.089). Both routes significantly outperformed controls (p < 0.01 and p < 0.05). Pharmacokinetics revealed exclusive lung tropism with peak concentrations at 5 min (1.9 × 103-5.1 × 104 PFU/organ) and phage levels falling below the limit of detection (<5 × 103 PFU/organ) within 24 h. Infected lungs showed significantly higher phage titres than uninfected ones, indicating in vivo replication. Safety studies showed no significant toxicity, immunogenicity, or local irritation. The integrated D29-based platform represents a comprehensive, integrated diagnostic-therapeutic solution covering the full "diagnosis-therapy" cycle. The test system provides rapid phenotypic drug susceptibility profiling, while the liposomal phage demonstrates potent therapeutic activity and favourable pharmacokinetics, supporting its clinical translation.
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