Fabrication of Capsaicin Loaded Nanocrystals: Physical Characterizations and In Vivo Evaluation

Abstract

Nano-crystallization is a new emerging strategy to promote the saturation solubility, dissolution rate and subsequent bioavailability of Biopharmaceutical Class II drugs. Capsaicin belongs to BCS class-II drugs having low water solubility and dissolution rate. Nano-crystals (NC) of pure Capsaicin was developed and optimized in order to increase its water solubility, dissolution and further to promote its adhesiveness to skin epidermis layer. NC formulations were subjected to stability studies, droplet size, surface charge, poly-dispensability index, drug content, entrapment efficiency, thermal analysis, surface morphology, crystalline studies, solubility profile, in vitro release and ex vivo permeation studies. In vivo anti-inflammatory assay (Carrageenan-induced paw edema) was performed in Sprague Dawley rats. Nanocrystals loaded with capsaicin showed particle size 120 ± 3.0 nm with surface charge of −20.7 ± 3.5 and PDI was 0.48 ± 1.5. Drug content and entrapment efficiency of T3 was 85% and 90 ± 1.9% respectively. Thermal studies predicted that melting peak of capsaicin was present in the formulation suggested that there was no interaction between active moieties and excipients in NC formulation. Surface morphology confirmed the presence of Nano-size crystals having rough crystalline surface. XRD proved that the capsaicin NC are successfully developed by using high speed homogenization. The solubility of capsaicin was found to be 12.0 ± 0.013 μg/mL in water. In vitro study revealed that 89.94 ± 1.9% of drug was released within 24 h. Similarly, drug permeation was 68.32 ± 1.83%, drug retained in skin was 16.13 ± 1.11% while drug retained on skin was 9.12 ± 0.14% after 12 h. The nanocrystals showed higher anti-inflammatory activity as compared to marketed product (Dicloran®). The study concluded that improvement in dissolution rate of capsaicin may potentially provide the opportunities in the development of a much cost-effective dosage forms that will produce improved pharmacological effects, but at low dose as compared to the already available products.

Promising photocatalytic and antimicrobial activity of novel capsaicin coated cobalt ferrite nanocatalyst

“…The XRD pattern indicates that the synthesized sample is in the nanoscale range. In addition, the diffraction peaks at 20.25 o and 28.0° corresponded to Capsaicin 44 , confirming the loading of capsaicin with the synthesized CoFe 2 O 4 NPs. The crystallite size of the synthesized NPs was caculated using Scherrer’s Equation 45 : where, D is the crystallite size, λ is the X-ray wavelength used, β is the full width at half maximum (FWHM) and θ is the diffraction angle.…”

Microencapsulation of Capsaicin in Chitosan Microcapsules: Characterization, Release Behavior, and Pesticidal Properties against Tribolium castaneum (Herbst)

“…Chitosan and its derivatives (i.e., CMCS) could be used in pesticide delivery, copolymeric concentration, and nanomicellar, which could effectively prevent ecological harm, including the photodegradation of the active ingredients [ 51 ]. In addition, chitosan could give the CAP loaded in microcapsules good solubility and permeation into the insect gut, causing a series of adverse reactions, such as delayed growth and development, decreased adult weight and reproduction rate, and even death [ 49 , 52 ]. This experiment further suggested that the CAP could significantly disturb the growth and development of the insects.…”

Optimization and Evaluation of Anti-Inflammatory Herbal Emulgel loaded with Vitex Negundo for Enhanced Permeation

“…Solution (1 mL) was taken, and PBS was used to dilute it up to 10 mL (pH 6.8). Using a UV-Visible Spectrophotometer at 273 nm, the drug content in emulgel was calculated spectrophotometrically (22,23). To determine the homogeneity of the drug content, experiments are carried out in triplicate (n = 3).…”