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]

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Summary

Introduction

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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