Sinha Priyam, Srivastava Shruti, Mishra Nidhi, Singh Dhananjay Kumar, Luqman Suaib, Chanda Debabrata, Yadav Narayan Prasad
a Department of Herbal Medicinal Products , CSIR - Central Institute of Medicinal and Aromatic Plants, PO CIMAP , Lucknow , UP , India ;
b Department of Molecular Bioprospection , CSIR - Central Institute of Medicinal and Aromatic Plants, PO CIMAP , Lucknow , UP , India.
Drug Dev Ind Pharm. 2016 Sep;42(9):1434-45. doi: 10.3109/03639045.2016.1141931. Epub 2016 Feb 15.
To develop and optimize nanoemulsion (NE)-based emulgel (EG) formulation as a potential vehicle for topical delivery of tea tree oil (TTO).
Central composite design was adopted for optimizing the processing conditions for NE preparation by high energy emulsification method viz. surfactant concentration, co-surfactant concentration, and stirring speed. The optimized NE was developed into emulgel (EG) using pH sensitive polymer Carbopol 940 and triethanolamine as alkalizer. The prepared EG was evaluated for its pH, viscosity, and texture parameters, ex vivo permeation at 37 °C and stability. Antimicrobial evaluation of EG in comparison to conventional gel and pure TTO was also carried out against selected microbial strains.
Optimized NE had particle size and zeta potential of 16.23 ± 0.411 nm and 36.11 ± 1.234 mV, respectively. TEM analysis revealed the spherical shape of droplets. The pH of EG (5.57 ± 0.05 ) was found to be in accordance with the range of human skin pH. EG also illustrated efficient permeation (79.58 μL/cm(2)) and flux value (JSS) of 7.96 μL cm(2)/h through skin in 10 h. Viscosity and texture parameters, firmness (9.3 ± 0.08 g), spreadability (2.26 ± 0.06 mJ), extrudability (61.6 ± 0.05 mJ), and adhesiveness (8.66 ± 0.08 g) depict its suitability for topical application. Antimicrobial evaluation of EG with same amount of TTO as conventional gel revealed broader zones of growth inhibitions against all the selected microbial strains. Moreover, EG was also found to be nonirritant (PII 0.0833). These parameters were consistent over 90 d.
TTO EG turned out to be a promising vehicle for the topical delivery of TTO with enhanced therapeutic efficacy.
开发并优化基于纳米乳(NE)的乳化凝胶(EG)制剂,作为茶树油(TTO)局部给药的潜在载体。
采用中心复合设计,通过高能乳化法优化纳米乳制备的工艺条件,即表面活性剂浓度、助表面活性剂浓度和搅拌速度。使用pH敏感聚合物卡波姆940和三乙醇胺作为碱化剂,将优化后的纳米乳制成乳化凝胶。对制备的乳化凝胶进行pH、粘度和质地参数评估,在37℃下进行离体渗透和稳定性评估。还对乳化凝胶与传统凝胶和纯TTO进行了抗菌评估,以对抗选定的微生物菌株。
优化后的纳米乳粒径和zeta电位分别为16.23±0.411nm和36.11±1.234mV。透射电镜分析显示液滴呈球形。乳化凝胶的pH值(5.57±0.05)符合人体皮肤pH值范围。乳化凝胶在10小时内通过皮肤的有效渗透率为79.58μL/cm²,通量值(JSS)为7.96μL cm²/h。粘度和质地参数,硬度(9.3±0.08g)、铺展性(2.26±0.06mJ)、挤出性(61.6±0.05mJ)和粘附性(8.66±0.08g)表明其适合局部应用。与传统凝胶中相同量的TTO相比,乳化凝胶的抗菌评估显示对所有选定的微生物菌株具有更宽的生长抑制区。此外,乳化凝胶也被发现无刺激性(PII 0.0833)。这些参数在90天内保持一致。
TTO乳化凝胶是一种有前景的TTO局部给药载体,具有增强的治疗效果。