Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies

Abstract

CB13 (1-Naphthalenyl[4-(pentyloxy)-1-naphthalenyl]methanone)-loaded poly(lactic-co-glycolic acid) nanoparticles (NPs) were produced by nanoprecipitation and tested for their in vitro release behavior and in vitro cytotoxicity assays. The effects of several formulation parameters such as polymer type, surfactant concentration, and initial drug amount were studied. NPs had a particle size 90-300 nm in diameter. Results obtained show that the main influence on particle size was the type of polymer employed during the particle production: the greater the hydrophobicity, the smaller the particle size. In terms of encapsulation efficiency (%), high values were achieved (∼68%-90%) for all formulations prepared due to the poor solubility of CB13 in the external aqueous phase. Moreover, an inverse relationship between release rate and NP size was found. On the other hand, low molecular weight and low lactide content resulted in a less hydrophobic polymer with increased rates of water absorption, hydrolysis, and erosion. NPs showed no cytotoxicity and may be considered to be appropriate for drug-delivery purposes.

Drug delivery of 6-bromoindirubin-3’-glycerol-oxime ether employing poly(d,l-lactide-co-glycolide)-based nanoencapsulation techniques with sustainable solvents

“…The zeta potential (ZP) of the NPs can prevent nanoparticle aggregation due to electrostatic repulsion [ 34 ]. Blank particles of all formulations showed comparable ZP between − 23.7 mV and − 27.3 mV similar to former studies [ 29 , 30 , 35 ]. An increase of the ZP was obtained for 6BIGOE-loaded NPs prepared by the EDE and PEG 400 method with values of − 15.5 mV and − 18.9 mV, respectively, whereas 6BIGOE-loaded NPs prepared by the Cyrene method showed a ZP similar to blank NPs (Fig.…”

Lipid nanocapsules decorated and loaded with cannabidiol as targeted prolonged release carriers for glioma therapy: In vitro screening of critical parameters

“…The choice of the oily phase was based on the solubility of CBD to easily achieve both high encapsulation efficiencies and drug loading. In this regard, whereas the authors that tried to encapsulate distinct cannabinoids in polymer nanoparticles only achieved encapsulation efficiencies around 70% [15,16,21], those studies that utilized lipid-based carriers exhibited values above 90% [17,22]. This comparison has been corroborated by Durán-Lobato et al [23].…”

“…In this context, these substances can take great advantage of nanomedicine-based formulation strategies. Consistently, several studies on nanocarriers encapsulating the different kinds of cannabinoids (phytocannabinoids [12][13][14], cannabidomimetics [15][16][17][18], and endocannabinoids [19]) have started being published with distinct therapeutic purposes. Notwithstanding that for cannabinoids to achieve high translational impact they should be devoid of psychoactive effects, the focus so far has been mainly put on the encapsulation of 9-delta-tetrahydrocannabinol (Δ 9 -THC) and its analogues.…”

An Integrative Review to Progress the Responsible Development of Nano-Drugs

“…Nanotechnology, mooted as a disruptive technology in the 4IR, represents materials with at least one dimension in nanometers (1-100nm) (Hartwig et al, 2021). These nanomaterials in the form of nanoparticles (NPs) display unusual properties, based on features like small size, improved surface area, reactive surface structure, robust chemical composition, good and selective solubility and varied shape (Banderas et al, 2012 andKazemzadeh et al, 2022). In the pharmaceutical industry, these properties are favourable because formulations including them are able to better control and regulate the pharmacodynamics (PD) and pharmacokinetics (PK) of drugs (Zhang et al, 2020) and deliver them to different parts of the body, specifically at the active site of the disease over a sustained period (Hartwig et al, 2021).…”