R&D Centre, Akay Bioactives, Akay Natural Ingredients Private Limited.
Biol Pharm Bull. 2024;47(9):1583-1593. doi: 10.1248/bpb.b24-00306.
The oleo-gum-resin of Boswellia serrata, an Ayurvedic herb for the treatment of chronic inflammatory diseases, contains both volatile (terpenes) and nonvolatile (boswellic acids) molecules as responsible for its bioactivity. The present randomized, double-blinded, placebo-controlled, crossover study evaluated the human pharmacokinetics of a 'natural' hybrid-hydrogel formulation of a unique full-spectrum boswellia extract (BFQ-20) (standardized for both volatile and nonvolatile bioactives) in comparison with unformulated extract (U-BE), for the first time. Mass spectrometry coupled with LC (UPLC-MS/MS) and gas chromatography (GC-MS/MS) measurements of the plasma concentration of boswellic acids and α-thujene at different post-administration time points followed by a single dose (400 mg) of U-BE and BFQ-20, to healthy volunteers (n = 16), offered 4-fold enhancement in the overall bioavailability of boswellic acids from BFQ-20, [area under the curve (AUC) (BFQ-20) = 9484.17 ± 767.82 ng * h/mL vs. AUC (U-BE) = 2365.87 ± 346.89 ng * h/mL], with the absorption maximum (T) at 6.3 h post-administration and elimination half-life (T) of 15.5 h (p < 0.001). While plasma α-thujene was not detectable upon U-BE administration, BFQ-20 provided significant absorption, [AUC (BFQ-20): 298.60 ± 35.48 ng * h/mL; C: 68.80 ± 18.60 ng/mL; T: 4.12 ± 0.38 h; T: 16.24 ± 1.12 h]. Further investigation of the anti-inflammatory effect revealed 70.5% inhibition of paw edema in rats compared to 38.0% for U-BE. In summary, the natural self-emulsifying reversible hybrid-hydrogel (N'SERH) formulation of boswellia extract using fenugreek mucilage (FenuMat) significantly increased the solubility (58-fold), stability, and bioavailability of both the volatile and non-volatile bioactives which in turn improved the anti-inflammatory efficacy of Boswellia extract.
乳香树的油脂树胶是一种阿育吠陀草药，用于治疗慢性炎症性疾病，其中包含挥发性（萜烯）和非挥发性（乳香酸）分子，这些成分负责其生物活性。本随机、双盲、安慰剂对照、交叉研究首次评估了一种独特的全谱乳香提取物（BFQ-20）的“天然”混合水凝胶配方（针对挥发性和非挥发性生物活性物质进行了标准化）的人体药代动力学，与未配方提取物（U-BE）进行比较，对健康志愿者（n=16）进行了单次剂量（400mg）的 U-BE 和 BFQ-20 给药，通过液相色谱-质谱联用（UPLC-MS/MS）和气相色谱-质谱联用（GC-MS/MS）测量给药后不同时间点的血浆中乳香酸和α-蒎烯的浓度，BFQ-20 中乳香酸的整体生物利用度提高了 4 倍，[BFQ-20 的 AUC（BFQ-20）=9484.17±767.82ngh/mL，与 AUC（U-BE）=2365.87±346.89ngh/mL]，吸收最大值（T）在给药后 6.3 小时，半衰期（T）为 15.5 小时（p<0.001）。虽然 U-BE 给药后未检测到血浆α-蒎烯，但 BFQ-20 提供了显著的吸收，[BFQ-20 的 AUC（BFQ-20）：298.60±35.48ng*h/mL；C：68.80±18.60ng/mL；T：4.12±0.38h；T：16.24±1.12h]。对抗炎作用的进一步研究表明，与 U-BE 相比，BFQ-20 可使大鼠足爪水肿抑制率达到 70.5%。综上所述，使用胡芦巴胶（FenuMat）的乳香提取物天然自乳化可逆混合水凝胶（N'SERH）配方显著提高了挥发性和非挥发性生物活性物质的溶解度（58 倍）、稳定性和生物利用度，从而提高了乳香提取物的抗炎功效。
