Abstract
Boswellic acids (BAs) are the main bioactive compounds of frankincense, a natural resin obtained from the genus Boswellia. This study aimed to develop a self-nanoemulsifying delivery system (SNEDS) to improve the antimicrobial and antiproliferative activities of standardized frankincense extract (Fr-extract). Fr-extract was standardized, and BA content was quantified using the developed HPLC-UV method. Screening studies of excipients followed by formula optimization using a mixture simplex lattice design was employed. The optimized Fr-SENDS formulation was characterized. Furthermore, microbiological and antiproliferative assessments of the standardized Fr-extract and Fr-SNEDS were evaluated. Quantification demonstrated that the major constituent is 11-keto-boswellic acid (KBA) (16.25%) among BA content (44.96%). The optimized Fr-SENDS (composed of 5% CapryolTM 90, 48.7% Gelucire® 44/14 and 46.3% ethanol) showed spherical nanosized dispersions with DS, PDI, and zeta potential of 17.9 nm, 0.2, and −14.5 mV, respectively. Fr-SNEDS exhibited lower MIC and MBC values compared with Fr-extract against pathogens conjugated with lung cancer and was comparable to reference antimicrobials. Fr-SNEDS showed superior antiproliferative activity over Fr-extract, with IC50 values of 20.49 and 109.5 μg mL−1, respectively. In conclusion, the optimized Fr-SNEDS could be easily developed and manufactured at a low cost and the in vitro results support its use as a potential adjuvant oral therapy for lung cancer. Further in vivo studies could be continued to assess the therapeutic efficiency of the prepared system.
Highlights
Nowadays, researchers are moving towards the utilization of phytoconstituents, owing to their therapeutic effectiveness with low side effects [1]
boswellic acids (BAs), a mixture comprised of four major triterpenes, namely β-boswellic acid (β-BA), 3acetyl-β-BA, 11-keto-boswellic acid (KBA), and 3-acetyl-11-keto-boswellic acid (AKBA),and two minors, namely α-boswellic acid (α-BA), and 3-acetyl-α-BA, were isolated from the oleogum resin of Boswellia species [1]
It is noteworthy that the retention times (Rt) of KBA and β-BA in the performed HPLC analysis are 2.5 and 6.5 min, respectively (Table 1), in agreement with those reported (2.6–3.4 and 7.5–8.6 min, respectively) [2]
Summary
Researchers are moving towards the utilization of phytoconstituents, owing to their therapeutic effectiveness with low side effects [1]. The major composition of the Boswellia resin shows approximately 50–60% of various BAs, and in herbal supplements, up to 65% [2] The analysis of these triterpenes is performed by different analytical methods based on HPLC-DAD [3] and LC/MS [1,4]. Boswellia triterpenoids were reported to have antitumor properties [7], apoptotic effects, and inhibited the protein synthesis in human leukemia cells [8] Both α- and β-KBA exhibited cytotoxicity against triple-negative breast cancer (TNBC) cell lines and induced in vivo apoptosis in MDA-MB-231 xenografts, where the β-isomers of KBA and AKBA demonstrated higher cytotoxic efficacies [5]. AKBA has an inhibitory effect on lipoxygenases following inhibition of cell proliferation [9]
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