Pterodon pubescens Benth (sucupira) microencapsulation influence on formulation stability outcome compared to non-encapsulated extract
Pterodon pubescens Benth (sucupira) microencapsulation influence on formulation stability outcome compared to non-encapsulated extract
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DOI：
10.1016/j.jddst.2021.102875
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发表时间：
2022-01-11
影响因子：
5
通讯作者：
Mazzola, Priscila Gava
中科院分区：
文献类型：
--
作者：
Giarola, Leila Regina;Coco, Julia Cedran;Mazzola, Priscila Gava
Pterodon pubescens Benth是巴西本土物种，用于民间医学缓解慢性疼痛。归因于该物种的抗炎、镇痛和抗增殖活性与在P. pubescens提取物中鉴定的vouacapans（呋喃二萜）和geranylgeraniol（无环二萜）具有直接关系。然而，很少有关于含有该物种的产品开发和稳定性研究的报告。这一差距促使对含有毛白杨微胶囊化提取物的卡波姆-940凝胶制剂与本文报告的非胶囊化提取物进行稳定性结果评价。用二氯甲烷提取种子，提供46.6%（w/w）的粗提取物产率。植物化学标记物通过具有二极管阵列检测器的高压液相色谱法（HPLC-DAD）和气相色谱-质谱联用（GC-MS）使用vouacapans 1：1比例异构体6 α-羟基-7 β-乙酰氧基vouacapan-17 β-酸甲酯和6 α-乙酰氧基-7 β-羟基-vouacapan-17 β-酸甲酯进行监测，用于定量和鉴定目的。以腰果胶为壁材制备了喷雾干燥微胶囊，扫描电镜（SEM）表征了微胶囊的结构，光散射参数表征了微胶囊的粒径分布。颗粒呈现双峰粒度分布，范围从0.2到500 μ m，vouacapans含量和包封率分别为55.6%和44.4%，总的喷雾干燥产率为82.6%（w/w）。含有微胶囊化提取物的制剂在测试条件下未达到可接受的结果，需要进一步研究进行优化。然而，在稳定性研究中，在25 ℃下避光储存的含有2.5%（w/v）未包封提取物的凝胶在180天内呈现出最佳结果。与凝胶基质制剂相比，在储存期间暴露于光下时，掺入的P. pubescens保持了流变学性质，具有更好的性能。该制剂通过合成膜递送vouacapans。该制剂是获得含有P. pubescens有益活性的新型局部凝胶基产品的第一步。
Pterodon pubescens Benth is a Brazilian native species, used in folk medicine for chronic pain relief. The anti-inflammatory, antinociceptive, and antiproliferative activities attributed to the species have a straight relationship with vouacapans (furanditerpenes) and geranylgeraniol (acyclic diterpenes), identified in P. pubescens extracts. Nevertheless, scarce reports are found on product development and stability studies containing this species. This gap prompted the stability outcome evaluation of carbomer-940 gel-based formulations containing P. pubescens microencapsulated extract compared to non-encapsulated extract reported herein. Seeds were extracted with dichloromethane providing 46.6% (w/w) crude extract yield. Phytochemical markers were monitored by High Pressure Liquid Chromatography with Diode Array Detector (HPLC-DAD) and Gas Chromatography coupled to Mass Detection (GC-MS) using the vouacapans 1:1 ratio isomers 6 alpha-hydroxy-7 beta-acetoxyvouacapan-17 beta-oate methyl ester and 6 alpha-acetoxy-7 beta-hydroxy-vouacapan-17 beta-oate methyl ester for quantification and identification purposes. Spray-dried microcapsules were produced with cashew gum as wall material with structure confirmed by scanning electron microscopy (SEM) and size distribution by light scattering parameters. The particles presented a bimodal size distribution ranging from 0.2 to 500 mu m, vouacapans content and encapsulation efficiency of 55.6% and 44.4% respectively, with an overall spray-drying yield of 82.6% (w/w). The formulation containing microencapsulated extract did not achieve an acceptable outcome under test condition, with further studies needed for optimization. Nevertheless, the gel containing 2.5% (w/v) of non-encapsulated extract stored at 25 degrees C protected from light presented the best results within 180 days in stability study. P. pubescens incorporation maintained rheological properties with better performance when exposed to light during storage time compared to the gel base formulation. The formulation delivered vouacapans throughout a synthetic membrane. This formulation is the first step to achieve a novel topical gel-based product containing P. pubescens beneficial activities.