Oral formulations for cannabidiol: Improved absolute oral bioavailability of biodegradable cannabidiol self-emulsifying drug delivery systems.

Aim: This study aimed to fabricate and evaluate three different SEDDS formulations to improve the oral bioavailability of cannabidiol (CBD). CBD has limited oral bioavailability due to its lipophilicity and extensive first-pass metabolism. By using different emulsifiers in the SEDDS formulations, this study seeks to optimize CBD loading capacities and enhance overall in vivo pharmacokinetic (PK) performance of CBD when administered orally.

Evaluation of the dissociation behavior of hydrophobic ion pairs via HPLC analysis.

Aim: The objective of this study was to investigate the stability of hydrophobic ion pairs (HIP) of tuftsin and perfluorooctanoic acid in physiological media via high performance liquid chromatography (HPLC).

Methods: HIP was formed between the model peptide tuftsin and perfluorooctanoic acid (PFOA). Precipitation efficiency and logP of HIP was determined via HPLC.

Optimizing hydrophilic drug incorporation into SEDDS using dry reverse micelles: a comparative study of preparation methods.

Aim: It was the aim of this study to compare two different dry reverse micelle (RM) preparation methods for the incorporation of hydrophilic drugs into oral self-emulsifying drug delivery systems (SEDDS).

Methods: Cationic ethacridine lactate, anionic fluorescein sodium salt and the antibiotic peptide bacitracin were solubilized in RM containing sodium docusate, soy phosphatidylcholine and sorbitan monooleate in highly lipophilic oils such as squalane. In the dry addition (DA) method, drugs were directly added to empty RM in their powder form.

Oral formulations for highly lipophilic drugs: Impact of surface decoration on the efficacy of self-emulsifying drug delivery systems.

Aim: To evaluate the impact of the surface decoration of cannabidiol (CBD) loaded self-emulsifying drug delivery systems (SEDDS) on the efficacy of the formulations to cross the various barriers faced by orally administered drugs.

Methods: Polyethylene glycol (PEG)-free polyglycerol (PG)-based SEDDS, mixed zwitterionic phosphatidyl choline (PC)/PEG-containing SEDDS and PEG-based SEDDS were compared regarding stability against lipid degrading enzymes, surface properties, permeation across porcine mucus, cellular uptake and cytocompatibility.

Results: SEDDS with a size of about 200 nm with narrow size distributions were developed and loaded with 20-21 % of CBD.

Phosphatase-degradable nanoparticles providing sustained drug release.

Aim: The study aimed to develop enzyme-degradable nanoparticles comprising polyphosphates and metal cations providing sustained release of the antibacterial drug ethacridine (ETH).

Methods: Calcium polyphosphate (Ca-PP), zinc polyphosphate (Zn-PP) and iron polyphosphate nanoparticles (Fe-PP NPs) were prepared by co-precipitation of sodium polyphosphate with cations and ETH. Developed nanocarriers were characterized regarding particle size, PDI, zeta potential, encapsulation efficiency and drug loading.

Counterion optimization for hydrophobic ion pairing (HIP): Unraveling the key factors.

In the present study, various surfactants were combined with insulin (INS), bovine serum albumin (BSA) and horseradish peroxidase (HRP) via hydrophobic ion pairing to increase lipophilicity and facilitate incorporation into self-emulsifying drug delivery systems (SEDDS). Lipophilicity of model proteins was successfully increased, achieving log D values up to 3.5 (INS), 3.

Hydrophobic Ion Pairing of Small Molecules: How to Minimize Premature Drug Release from SEDDS and Reach the Absorption Membrane in Intact Form.

The present work aimed to form hydrophobic ion pairs (HIPs) of a small molecule remaining inside the oily droplets of SEDDS to a high extent. HIPs of ethacridine and various surfactants classified by functional groups of phosphates, sulfates, and sulfonates were formed and precipitation efficiency, log D, and solubility in different excipients were investigated. Most lipophilic HIPs were incorporated into SEDDS and evaluated regarding drug release.

Surface design of nanocarriers: Key to more efficient oral drug delivery systems.

As nanocarriers (NCs) can improve the solubility of drugs, prevent their degradation by gastrointestinal (GI) enzymes and promote their transport across the mucus gel layer and absorption membrane, the oral bioavailability of these drugs can be substantially enhanced. All these properties of NCs including self-emulsifying drug delivery systems (SEDDS), solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), liposomes, polymeric nanoparticles, inorganic nanoparticles and polymeric micelles depend mainly on their surface chemistry. In particular, interaction with food, digestive enzymes, bile salts and electrolytes, diffusion behaviour across the mucus gel layer and fate on the absorption membrane are determined by their surface.