Neolupenol and Antiinflammatory Activity

Neolupenol, a pentacyclic triterpene isolated from Pluchea lanceolata flowers, was studied to determine its anti-inflammatory activity against carrageenin-induced rat-paw edema. The degree of edema inhibition was found to increase with dose as well as time interval and was found to be maximum at 300 min. Neolupenol, when administered at 100 mg/kg, p.o. was found to exhibit 70% edema inhibition which was greater than that of the reference compound, ibuprofen (50 mg/kg, p.o., 65% inhibition, 300 min).     

Pharmacotherapeutic management of macular edema in diabetic subjects undergoing cataract surgery

ABSTRACT

Introduction: Cataracts and diabetes are widespread pathologies that are of growing concern to the global population. In diabetic patients who have had cataract surgery, the worsening of preexisting diabetic macular edema or occurrence of pseudophakic cystoid macular edema are common causes of visual impairment even with the most advanced surgical techniques available today for phacoemulsification.

Areas covered: In this review, the authors assess the available literature to evaluate and compare different drugs, with the aim of establishing the best pharmacological strategies for the prevention and treatment of macular edema in diabetic patients undergoing cataract surgery.

Expert opinion: Guidelines for the optimal management of diabetic macular edema in conjunction with cataract surgery or treatment of pseudophakic cystoid macular edema in diabetic patients are still lacking. To treat these conditions, clinicians need to understand the pharmacokinetics, posology, and efficacy of available drugs: topical non-steroidal anti-inflammatory drugs (NSAIDs), intravitreal anti-vascular endothelial growth factors (VEGFs), and both topical and intravitreal steroids. Diabetic patients undergoing cataract surgery should receive topical NSAIDs to prevent pseudophakic cystoid macular edema. Intravitreal anti-VEGFs and steroids, in association with cataract surgery, are indicated for patients with preexisting diabetic macular edema or those at high risk of macular edema after surgery.     

Effect of aliskiren addition to amlodipine on ankle edema in hypertensive patients: a three-way crossover study

Objective: The aim of this study was to assess the effect of aliskiren and amlopidine on ankle-foot volume (AFV) and pretibial subcutaneous tissue pressure (PSTP).

Research design and methods: After 4-week placebo, 120 outpatients with grade 1 – 2 hypertension were randomized to amlodipine 10 mg or aliskiren 300 mg or their combination for 8 weeks in three crossover periods. At the end of each treatment, blood pressure, AFV, PSTP, plasma renin activity (PRA) and norepinephrine were assessed.

Results: Both monotherapies similarly reduced systolic blood pressure (SBP; p < 0.001) and diastolic blood pressure (DBP; p < 0.001), but the reduction was greater with amlodipine/aliskiren combination (SBP: - 24.6 mmHg, p < 0.001 vs monotherapy; DBP: -20.9 mmHg, p < 0.01 vs monotherapy). Amlodipine increased both AFV (+ 28.4%, p < 0.01) and PSTP (+ 80.4%, p < 0.01), while the combination produced a less marked increase in AFV (+ 6.6%, p < 0.01 vs amlodipine) and PSTP (+ 20.1%, p < 0.01 vs amlodipine). Plasma norepinephrine increased with amlodipine (+ 53.5%, p < 0.01) and this increase was not reduced by aliskiren addition. PRA was unaffected by amlodipine, while it was reduced by both aliskiren monotherapy (- 77.7%, p < 0.01) and aliskiren/amlodipine combination (- 75.7%, p < 0.01).

Conclusions: Direct renin inhibition by aliskiren partially counteracts the microcirculatory changes responsible for calcium-channel-induced edema formation, possibly through preferential vasodilation of venous capacitance vessels.     

己美舒利对大鼠脑损伤后脑水肿及髓过氧化物酶、金属蛋白酶-2的影响

目的阐明环氧化酶-2（cox-2）抑制剂尼美舒利对大鼠创伤性脑损伤的影响与机制。方法健康雄性SD大鼠40只,随机分为4组：对照组、尼美舒利组【6mg／（kg·d）1、创伤组、创伤＋尼美舒利组f6mg／（kg·d）1。利用300g,／m的自由落体重力打击装置创建SD大鼠创伤性脑损伤模型,创伤后24h进行神经功能评分,随后处死动物并断头取脑组织。脑水肿及血脑屏障通透性分别以干湿重称重法及伊文思蓝染色测定,测量脑组织中髓过氧化物酶（MPO）及金属蛋白酶-2（MMP-2）的含量以及病理组织形态学观察。结果创伤组脑组织含水量及EB含量比对照组明显增加（P〈0．05）,创伤＋尼美舒利组脑组织含水量及EB含量比创伤组明显减少（P〈0．01）。创伤＋尼美舒利组脑组织MMP-2、MPO表达比创伤组减少,MPO蛋白表达与MMP-2蛋白表达呈正相关。结论在创伤性脑损伤大鼠模型中,尼美舒利通过保持血脑屏障完整性,抑制MPO、MMP-2的过度表达（可能通过其抗炎能力）而发挥其神经保护作用。     

Delivery of steroids into the eye for the treatment of macular edema

ABSTRACT

Introduction: Steroids have been in extensive use in ophthalmology since their discovery in 1948. Steroids are effective for the treatment of macular edema and may be delivered into the eye either topically, systemically, subconjunctivally, sub-Tenon, intravitreally and through injectable sustained release devices. Various steroid formulations and devices are commercially available. Each carries advantages and disadvantages, which requires the ophthalmologist to exercise careful medical judgment upon treatment selection.

Areas covered: This article focuses in steroid delivery into the eye for the treatment of macular edema, and reviews the current and future treatment options, summarizing their clinical efficacy and possible adverse effects.

Expert opinion: Steroids have an important role in the treatment of macular edema, regardless of its cause. Steroids are efficacious, low-cost, and much clinical experience has been accumulated regarding their use over the years. Prolonged systemic steroid use may be associated with severe systemic and local side effects, directly proportional to dosage and time. Intravitreal delivery of steroids has gained popularity as the medication is administered close to the target tissue, significantly reducing the possibility of systemic adverse effects. The biggest problem associated with intravitreal steroids still remains unacceptably high risk of glaucoma and cataract formation. Various controlled-release intravitreal delivery devices are currently commercially available, and more are in the pipeline. While they still carry the risk of local side effects, they are efficacious and can control macular edema for months and years after a single administration.     

Optimization of novel tocopheryl acetate nanoemulsions for parenteral delivery of curcumin for therapeutic intervention of sepsis

Objective: The objective of this study is to develop a nanostructured parenteral delivery system, laden with curcumin (CUR), for the therapeutic intervention of sepsis and associated pathologies.

Methods: Nanoemulsions were fabricated using sonication and speed homogenization. Size and zeta potential were evaluated by dynamic light scattering and transmission electron microscopy analysis. Pharmacodynamic and pharmacokinetic studies were performed on a rat model of lipopolysaccharide (LPS)-induced sepsis.

Results: The drug content of optimized nanoemulsion (F5) formulation (particle size 246 ± 08 nm, polydispersity index (PDI) of 0.120, zeta potential of ?41.1 ± 1.2 mV) was found to be 1.25 mg/ml. In vitro release studies demonstrated that F5 was able to sustain the release of CUR for up to 24 h. Minimal hemolysis and cellular toxicity demonstrated its suitability for intravenous administration. Significant reduction of inflammatory mediator levels was mediated through enhanced uptake by in RAW 264.7 and THP-1 in absence/presence of LPS. Nanoemulsion resulted in an improvement of plasma concentration (AUC_F5/AUC _CUR = 8.80) and tissue distribution of CUR in rats leading to a reduction in LPS-induced lung and liver injury due to less neutrophil migration, reduced TNF-α levels and oxidative stress (demonstrated by levels of lipid peroxides as well as carbonylated proteins) as confirmed by histopathological studies.

Conclusion: The findings suggest that the therapeutic performance (i.e., reduction in oxidative damage in tissues) of CUR can be enhanced by employing tocol acetate nanoemulsions (via improving pharmacokinetics and tissue distribution) as a platform for drug delivery in sepsis-induced organ injury.     

视网膜中央静脉阻塞合并黄斑水肿的中西医治疗进展

视网膜中央静脉阻塞(Central Retinal Vein Occlusion,CRVO)容易并发多种合并症,其中黄斑水肿最为多见,常导致比较严重的视力下降。由于它对视力的严重损害以及对患者生活质量的严重影响,寻求更有效的治疗方法具有重大的现实意义。本文从中医治疗、西医治疗及中西结合治疗等3个方面阐述了视网膜静脉阻塞合并黄斑水肿的治疗近况,并提出了视网膜静脉阻塞合并黄斑水肿未来治疗的展望。     

活血熄风通络汤联合西医治疗脑出血后脑水肿随机平行对照研究

[目的]观察活血熄风通络汤联合西医治疗脑出血后脑水肿疗效。[方法]使用随机平行对照方法,将110例住院患者按病志号抽签法简单随机分为两组。对照组55例甘露醇,0.2g甘露醇+20m L葡萄糖,1次/d,静注;速尿片,0.4g/次,1次/d。治疗组活血熄风通络汤(天麻、白芷、益母草各10g,川芎、大黄各8g,三七粉、地龙各6g,全蝎5g),1剂/d,水煎150m L,早晚口服;西医治疗同对照组。观测临床症状、血肿大小、水肿体积、NIHSS评分、ADL评分、不良反应。连续治疗2疗程,判定疗效。[结果]治疗组显效26例,有效25例,无效4例,总有效率92.73%。对照组显效16例,有效24例,无效15例,总有效率72.73%。治疗组疗效优于对照组(P0.05)。血肿大小、水肿体积、NIHSS评分及ADL评分改善治疗组优于对照组(P0.05)。[结论]活血熄风通络汤联合西医治疗脑出血后脑水肿效果显著,值得推广。     

自拟中药方湿热敷对湿热下注型混合痔术后消肿止痛作用的临床观察

目的观察自拟中药方湿热敷对湿热下注型混合痔(内痔Ⅲ期)术后的消肿止痛作用。方法将88例湿热下注型混合痔(内痔Ⅲ期)术后患者随机分为治疗组和对照组,每组44例。治疗组于术后用自拟中药方湿热敷,对照组用痔疾洗液湿热敷。两组疗程均为14天,分别于术后第2天、第7天、第14天观察出血、疼痛、渗液、充血及外痔水肿情况,并于疗程结束后评价临床疗效。结果①治疗组、对照组总有效率均为100%,组间临床疗效差异有统计学意义(P0.05)。②治疗组术后第7天与第2天比较,渗液、充血分级积分差异有统计学意义(P0.05);第14天与第7天比较,出血、疼痛、渗液、充血分级积分差异有统计学意义(P0.05)。对照组术后第7天与第2天比较,充血分级积分差异有统计学意义(P0.05);第14天与第7天比较,出血、疼痛、渗液、充血分级积分差异有统计学意义(P0.05)。组间比较,第7天、第14天疼痛、渗液、充血分级积分差异有统计学意义(P0.05)。③治疗组、对照组术后第7天与第2天、第14天与第7天、第14天与第2天比较,水肿面积差异均有统计学意义(P0.05)。结论自拟中药方可明显减轻湿热下注型混合痔(内痔Ⅲ期)术后患者的肛门出血、疼痛、渗液、充血、水肿等术后症状,临床疗效优于痔疾洗液。