Update on actinic keratosis in clinical trial experience with imiquimod

Actinic keratoses (AK) is a sun induced cutaneous lesion, currently considered as a squamous cell carcinoma in situ that has the potential to progress to invasive SCC. To treat them, numerous, ablative and no ablative, therapeutic approaches exist. Among them, imiquimod, a toll like receptor agonist, recently approved to treat them in the US and Europe, has demonstrated to be effective and safe with an acceptable tolerability in the treatment of these lesions. In this article the results of several high quality RCT are analysed.     

咪喹莫特脂质体与乳膏体外经皮扩散行为的比较

采用中和法制备咪喹莫特脂质体，研究了其体外经皮扩散行为并与咪喹莫特乳膏进行比较。制得的脂质体平均粒径为855nm，跨距为1．65，能经皮缓慢扩散，皮层的局部贮药量比之乳膏有增加，可减少药物全身吸收。     

咪喹莫特在尖锐湿疣治疗中的应用

咪喹莫特是一种局部应用的免疫调节剂 ,可刺激皮肤粘膜产生干扰素、肿瘤坏死因子和白介素 1,6,8,提高细胞免疫应答 ,产生抗病毒效果。5 %咪喹莫特霜治疗尖锐湿疣 ,疣体完全清除率为37%～ 5 0 % ,不良反应为局部轻、中度的瘙痒、红斑、烧灼感、触痛、溃疡、糜烂、疼痛等 ,具有较好临床应用价值。     

5%咪喹莫特乳膏治疗外阴鳞状上皮内瘤样病变的疗效及安全性分析

目的探讨5%咪喹莫特乳膏治疗外阴鳞状上皮内瘤样病变（VIN）的疗效和安全性。方法对42例门诊就诊的VIN患者给予5%咪喹莫特乳膏治疗,逐渐增加用药量至每周外用4次,疗程16周,期间每2周复诊1次,观察皮损变化及不良反应情况。疗程结束后再次行组织病理检查。结果实际完成疗程者36例,其中痊愈21例,好转10例,总有效率为86.1%。VINⅠ、VINⅡ的治愈率明显高于VINⅢ,VINⅠ的有效率也高于VINⅢ。好转患者皮损面积平均缩小57.2%。在治疗过程中,没有患者疾病进展或被诊断为鳞癌。20例患者出现不同程度的不良反应,主要表现为轻、中度的局部刺激症状,无一例患者出现系统症状,减量或暂时停药2周后均恢复正常治疗。结论外用5%咪喹莫特乳膏治疗VIN安全有效,患者耐受性好。     

Pigmented condyloma acuminatum

We herein report a case of pigmented condyloma acuminatum in the genital region. A histopathological examination revealed keratinocyte proliferation, papillomatosis and basal pigmentation. Cellular atypia was rarely observed. The patient also had ordinary skin‐colored nodules on the coronal sulcus. Polymerase chain reaction amplification with consensus primers for human papillomavirus (HPV) and subsequent sequencing confirmed an infection of HPV type 6. Pigmented condyloma acuminatum is not rare; however, making the differential diagnosis between bowenoid papulosis and seborrheic keratosis is sometimes difficult. The mechanism of pigmentation in such cases remains unknown and requires further investigation. HPV typing is a useful method for diagnosing the disease.     

基于pH梯度载药技术的咪喹莫特脂质体的制备工艺研究

目的 根据咪喹莫特的理化性质,利用pH梯度主动载药技术制备脂质体,考察其性状、粒径、表面电荷及体外释药特征。方法 葡聚糖凝胶滤过法测定脂质体的包封率,以包封率与成型性为主要指标筛选制备方法,考察水化液的种类、pH值、离子强度及pH梯度载药、磷脂-胆固醇比例、脂药比、维生素E用量对包封率的影响;正交试验优化咪喹莫特脂质体的处方,考察脂质体样品在0~4℃下的稳定性。结果 按处方咪喹莫特50 mg、大豆卵磷脂400 mg、胆固醇130 mg、油酸10 mg、维生素E 5 mg、柠檬酸pH 2.5缓冲液5 mL,采用薄膜分散法工艺制备脂质体样品,并进行pH梯度主动载药,pH值调至7.0。制得的咪喹莫特脂质体呈白色均匀的混悬液,脂质体微粒圆整,分散性好,粒径（347±21）nm,包封率（81.2±1.9）%,Zeta电位（-12.19±1.7）mV。结论 pH梯度主动载药技术适于咪喹莫特脂质体的制备。