Lyophilized Drug-Loaded Solid Lipid Nanoparticles Formulated with Beeswax and Theobroma Oil

Abstract

Solid lipid nanoparticles (SLNs) have the potential to enhance the systemic availability of an active pharmaceutical ingredient (API) or reduce its toxicity through uptake of the SLNs from the gastrointestinal tract or controlled release of the API, respectively. In both aspects, the responses of the lipid matrix to external challenges is crucial. Here, we evaluate the effects of lyophilization on key responses of 1:1 beeswax–theobroma oil matrix SLNs using three model drugs: amphotericin B (AMB), paracetamol (PAR), and sulfasalazine (SSZ). Fresh SLNs were stable with sizes ranging between 206.5–236.9 nm. Lyophilization and storage for 24 months (4–8 °C) caused a 1.6- and 1.5-fold increase in size, respectively, in all three SLNs. Zeta potential was >60 mV in fresh, stored, and lyophilized SLNs, indicating good colloidal stability. Drug release was not significantly affected by lyophilization up to 8 h. Drug release percentages at end time were 11.8 ± 0.4, 65.9 ± 0.04, and 31.4 ± 1.95% from fresh AMB-SLNs, PAR-SLNs, and SSZ-SLNs, respectively, and 11.4 ± 0.4, 76.04 ± 0.21, and 31.6 ± 0.33% from lyophilized SLNs, respectively. Thus, rate of release is dependent on API solubility (AMB < SSZ < PAR). Drug release from each matrix followed the Higuchi model and was not affected by lyophilization. The above SLNs show potential for use in delivering hydrophilic and lipophilic drugs.

Formulation of Cinnamon (Cinnamomum verum) oil loaded solid lipid nanoparticles and evaluation of its antibacterial activity against Multi-drug Resistant Escherichia coli

“…Nowadays, the effectiveness of a drug substance depends not only on the properties of the drug but also on the carrier system, which may lead to the controlled and localized release of the active substance based on specific clinical goals [17]. Solid lipid nanoparticles (SLNs) have been recommended as a new drug delivery carrier, mainly for lipophilic active ingredients [18] that can physically protect sensitive drugs (oxidation, light, humidity) and provide a controlled drug release, high surface area to volume ratio, and high drug loading capacity [19,20]. They are composed of solid biodegradable lipids in aqueous colloidal dispersions, unifying the benefits of liposomes and fat emulsions simultaneously [21].…”

Next-generation materials for RNA–lipid nanoparticles: lyophilization and targeted transfection

“…As for adverse effect of cryoprotectant usage for storage of RNA-LNPs, the size of RNA-LNPs enhances more or less after reconstruction of freeze-dried RNA-LNPs. The cryoprotectants that have been evaluated for the freeze-drying of LNPs include monosaccharides (glucose, 40–44 fructose, 41–43,45 mannitol, 1,44,46–53 mannose, 40,43–45 sorbitol, 41,44,46,47 and xylose 45 ), disaccharides (sucrose, 1,23,24,40,42,45,52,54–57 lactose, 44,45 maltose, 23,40,42,44,54 and trehalose 1,24,40,44,46,47,53,54,56,58–60 ), polysaccharides (raffinose), 45 hydrophilic polymers (polyvinylpyrrolidone (PVP), 44,46,47 polyvinyl alcohol (PVA), 44,51 and gelatin 44 ), and hydrophilic chemicals (glycine, 44,46,47 ) (Table 2).…”

The Fundamental Role of Lipids in Polymeric Nanoparticles: Dermal Delivery and Anti-Inflammatory Activity of Cannabidiol

“…For example, gold nanoparticles were shown to permeate through pig skin due to their nanoscale size [ 17 ], whereas polymeric nanoparticles such as PLGA-NPs additionally enhanced the permeation of flufenamic acid through the skin by a change in the local pH that mediates the hydrolytic degradation rate of the polymer [ 18 ]. Another report showed that the release profiles of solid lipid nanoparticles (SLNs) prepared with a combination of theobroma oil and beeswax were depended on the melting point of the components [ 19 ]. In a release study performed at 37 °C, initial quick release rates of loaded drugs were associated with theobroma oil having a melting point between 34–38 °C, whereas further slower release rates were associated with beeswax’s melting point of 63–67 °C.…”