Evaluation of In Vitro Capsaicin Release and Antimicrobial Properties of Topical Pharmaceutical Formulation

Abstract

(1) Background: Capsaicin is the main capsaicinoid of the Capsicum genus and it is responsible for the pungent taste. Medical uses of the fruits of chili peppers date from the ancient time until nowadays. Most of all, they are used topically as analgesic in anti-inflammatory diseases as rheumatism, arthritis and in diabetic neuropathy. Reports state that the Capsicum genus, among other plant genera, is a good source of antimicrobial and antifungal compounds. The aim of this study was the preparation of a pharmaceutical Carbopol-based formulation containing capsaicin and the evaluation of its in vitro release and antimicrobial and antifungal properties. (2) Methods: It was first stabilized with an extraction method from the Capsicum annuum fruits with 98% ethanol and then the identification and determination of Capsaicin in this extract was realized by HPLC. (3) Results and Conclusions: Rheological analyses revealed that the selected formulation exhibited a pseudo-plastic behavior. In vitro release studies of capsaicin from a Carbopol-based formulation reported that approximately 50% of capsaicin was release within 52 h. Additionally, the Carbopol-based formulation significantly increased the antimicrobial effects of capsaicin towards all tested bacteria and fungi strains.

Lactobacillus rhamnosus attenuates Thai chili extracts induced gut inflammation and dysbiosis despite capsaicin bactericidal effect against the probiotics, a possible toxicity of high dose capsaicin

“…Furthermore, capsaicin in the very high dose (2 mM) reduced enterocyte viability and demonstrated bactericidal effect on L . rhamnosus GG supporting cytotoxicity and bactericidal activity of capsaicin [ 14 , 80 – 82 ]. Hence, gut barrier defect from the high dose chili extracts might be partly responsible from the direct enterocyte cytotoxicity of capsaicin that induced local inflammation (colon cytokines; TNF-α and IL-6) and loose stool.…”

Pharmacological Properties and Health Benefits of Capsicum Species: A Comprehensive Review

“…Researchers have recently stated that some varieties of chili peppers and their active compounds exhibit significant antimicrobial properties, equivalent to some modern-day antibiotics [73][74][75][76]. Especially, Goci et al investigated the carbopol-based formulated capsaicin enhances the antibacterial and antifungal effects against Escherichia coli (ATCC 10536), Bacillus cereus (Peru MycA 4), Salmonella typhi (Peru Myc 7), Staphylococcus aureus (ATCC 6538), Candida tropicalis (YEPGA 6184), Candida albicans (YEPGA 6379), Candida parapsilosis (YEPG 6551), and Candida albicans (YEPGA 6183), with a minimum inhibitory concentration (MIC) value reduction of at least 50% [77].…”

Capsicum annuum L. and its bioactive constituents: A critical review of a traditional culinary spice in terms of its modern pharmacological potentials with toxicological issues

“…The ethanol solution extract of C. annuum fruits was used for Carbopol‐based formulation containing capsaicin where the release of the capsaicin was 50% within 52 hr. Moreover, the in vitro drug release study of the same via dialyzes membrane method and the capsaicin and Carbopol formulation showed significant antimicrobial activity at a concentration range of 0.312–10 μg/ml against a wide variety of bacterial strains namely E. coli (ATCC 10536), Bacillus cereus (Peru MycA 4), Salmonella typhi (Peru Myc 7), S. aureus (ATCC 6538); Candida tropicalis (YEPGA 6184), Candida albicans (YEPGA 6379), Candida parapsilosis (YEPG 6551) C. albicans (YEPG 6138), C. parapsilosis (ATCC 22019), and Candida krusei (ATCC 6258) (Goci et al, 2021). The ethanol solution extract of C. annuum showed a zone of inhibition (6.33 ± 0.58 mm) reflecting efficient antibacterial activity against Streptococcus pneumoniae (Ďúranová et al, 2021).…”