Mishra Nidhi, Rai Vineet Kumar, Yadav Kuldeep Singh, Sinha Priyam, Kanaujia Archana, Chanda Debabrata, Jakhmola Apurva, Saikia Dharmendra, Yadav Narayan Prasad
Botany and Pharmacognosy Department, CSIR-Central Institute of Medicinal and Aromatic Plants, P.O. CIMAP, Lucknow, 226015, India.
Molecular Bioprospection Department, CSIR-Central Institute of Medicinal and Aromatic Plants, P.O. CIMAP, Lucknow, 226015, India.
AAPS PharmSciTech. 2016 Apr;17(2):482-92. doi: 10.1208/s12249-015-0378-x. Epub 2015 Aug 8.
Mentha spicata L. var. viridis oil (MVO) is a potent antifungal agent, but its application in the topical treatment is limited due to its irritancy and volatility. It was aimed to develop more efficient, chitosan-incrusted MVO microspheres with reduced volatility and lesser irritancy and to dispense it in the form of ointment. Simple coacervation technique was employed to microencapsulate MVO in chitosan matrix. Morphological properties and polymer cross-linking were characterized by scanning electron microscopy and differential scanning calorimetry, respectively. Optimization was carried out on the basis of entrapment efficiency (EE) using response surface methodology. Well-designed microspheres having smooth surface and spherical shape were observed. EE (81.20%) of optimum batch (R21) was found at 1.62% w/v of cross-linker, 5.4:5 of MVO to chitosan ratio and at 1000 rpm. R21 showed 69.38 ± 1.29% in vitro MVO release in 12 h and 96.92% retention of MVO in microspheres even after 8 week. Ointments of PEG 4000 and PEG 400 comprising MVO (F1) and R21 (F2) were developed separately. F2 showed comparatively broader zone of growth inhibition (13.33 ± 1.76-18.67 ± 0.88 mm) and less irritancy (PII 0.5833, irritation barely perceptible) than that of F1. F2 was able to avoid the direct contact of mild irritant MVO with the skin and to reduce its rapid volatility. Controlled release of MVO helped in lengthening the duration of availability of MVO in agar media and hence improved its therapeutic efficacy. In conclusion, a stable and non-irritant formulation with improved therapeutic potential was developed.
留兰香变种绿薄荷油(MVO)是一种有效的抗真菌剂,但其在局部治疗中的应用因刺激性和挥发性而受到限制。目的是开发更高效、壳聚糖包埋的MVO微球,以降低挥发性并减少刺激性,并将其制成软膏形式。采用简单的凝聚技术将MVO微囊化于壳聚糖基质中。分别通过扫描电子显微镜和差示扫描量热法对形态学性质和聚合物交联进行表征。使用响应面法基于包封率(EE)进行优化。观察到设计良好的微球表面光滑且呈球形。在交联剂浓度为1.62%(w/v)、MVO与壳聚糖比例为5.4:5以及转速为1000 rpm时,最佳批次(R21)的EE为81.20%。R21在12小时内的体外MVO释放率为69.38±1.29%,即使在8周后,微球中MVO的保留率仍为96.92%。分别制备了含MVO的聚乙二醇4000和聚乙二醇400软膏(F1)以及含R21的软膏(F2)。与F1相比,F2显示出相对更宽的生长抑制区(13.33±1.76 - 18.67±0.88 mm)和更低的刺激性(PII 0.5833,刺激几乎不可察觉)。F2能够避免轻度刺激性的MVO与皮肤直接接触,并降低其快速挥发性。MVO的控释有助于延长MVO在琼脂培养基中的可用时间,从而提高其治疗效果。总之,开发了一种具有改善治疗潜力的稳定且无刺激性的制剂。