Application of biorelevant in vitro assays for the assessment and optimization of ASD-based formulations for pediatric patients.

Amorphous solid dispersions (ASD) have been a successful formulation strategy to overcome the poor aqueous solubility of many novel drugs, but the development of pediatric formulations presents a special challenge due to variable gastrointestinal conditions in children. It was the aim of this work to design and apply a staged biopharmaceutical test protocol for the in vitro assessment of ASD-based pediatric formulations. Ritonavir was used as a model drug with poor aqueous solubility.

Development and Characterization of -Propyl Gallate Encapsulated Solid Lipid Nanoparticles-Loaded Hydrogel for Intranasal Delivery.

The objective of the present study was to develop -propyl gallate-loaded solid lipid nanoparticles (PG-SLNs) in a hydrogel (HG) formulation using Transcutol-P (TC-P) as a permeation enhancer. Modified solvent injection technique was applied to produce optimized PG-SLNs via the Quality by Design approach and central composite design. The in vitro mucoadhesion, scavenging activity, drug release, permeation studies of PG from PG-SLNs-loaded HG were evaluated under simulated nasal conditions.

A comparison study of lipid and polymeric nanoparticles in the nasal delivery of meloxicam: Formulation, characterization, and in vitro evaluation.

With the increasingly widespread of central nervous system (CNS) disorders and the lack of sufficiently effective medication, meloxicam (MEL) has been reported as a possible medication for Alzheimer's disease (AD) management. Unfortunately, following the conventional application routes, the low brain bioavailability of MEL forms a significant limitation. The intranasal (IN) administration route is considered revolutionary for CNS medications delivery.

Regulatory status quo and prospects for biosurfactants in pharmaceutical applications.

The concept of going 'green' and 'cold' has led to utilizing renewable resources for the synthesis of microbial biosurfactants that are both patient and eco-friendly. In this review, we shed light on the potential and regulatory aspects of biosurfactants in pharmaceutical applications and how they can significantly contribute to novel concepts for the Coronavirus 2019 (COVID-19) vaccine and future treatment. We emphasize that more specific guidelines should be formulated to regulate the approval of biosurfactants for human use.

Regulatory Considerations, Challenges and Risk-based Approach in Nanomedicine Development.

The translation of nanomedicines from the lab level into marketed product faces several challenges, including characterization of physicochemical properties, pharmacodynamics, pharmacokinetics, process control, biocompatibility, and nanotoxicity, scaling-up as well as reproducibility. The challenges of nanomedicine development are in connection with the different requirements from the patient (clinical and therapeutic use), industry (production), and regulatory bodies (authorization process). This paper aims at reviewing the status and regulatory aspects of nano-based drug delivery systems with a focus on the Food and Drug Administration (FDA) and the European Medicine Agency (EMA) regulations.

The Effect of Counterions in Hydrophobic Ion Pairs on Oral Bioavailability of Exenatide.

The aim of this study was to evaluate the potential of -octadecyl sulfate (SOS) as a counterion for hydrophobic ion pairing (HIP) with exenatide-a potent glucagon-like peptide-1 (GLP-1) analogue in the treatment of diabetes mellitus-to improve its oral bioavailability. Exenatide was ion-paired with SOS and docusate (DOC) serving as the gold standard followed by the incorporation in a self-emulsifying drug delivery system (SEDDS) comprising Capmul MCM EP, Captex 355, Kolliphor RH40, and propylene glycol at a mass ratio of 41:15:40:4. The hydrophobicity of exenatide-SOS and exenatide-DOC was characterized by determining the butanol-water partition coefficient (log ).

Hydrophobic ion pairing of a GLP-1 analogue for incorporating into lipid nanocarriers designed for oral delivery.

The lipophilic character of peptides can be tremendously improved by hydrophobic ion pairing (HIP) with counterions to be efficiently incorporated into lipid-based nanocarriers (NCs). Herein, HIPs of exenatide with the cationic surfactant tetraheptylammonium bromide (THA) and the anionic surfactant sodium docusate (DOC) were formed to increase its lipophilicity. These HIPs were incorporated into lipid based NCs comprising 41% Capmul MCM, 15% Captex 355, 40% Cremophor RH and 4% propylene glycol.

Progress and perspectives of brain-targeting lipid-based nanosystems via the nasal route in Alzheimer's disease.

Since health care systems dedicate substantial resources to Alzheimer's disease (AD), it poses an increasing challenge to scientists and health care providers worldwide, especially that many decades of research in the medical field revealed no optimal effective treatment for this disease. The intranasal administration route seems to be a preferable route of anti-AD drug delivery over the oral one as it demonstrates an ability to overcome the related obstacles reflected in low bioavailability, limited brain exposure and undesired pharmacokinetics or side effects. This delivery route can bypass the systemic circulation through the intraneuronal and extraneuronal pathways, providing truly needleless and direct brain drug delivery of the therapeutics due to its large surface area, porous endothelial membrane, the avoidance of the first-pass metabolism, and ready accessibility.

Nose-to-brain delivery of antiglioblastoma drugs embedded into lipid nanocarrier systems: status quo and outlook.

Glioblastoma multiforme (GBM) is one of the most devastating and deadly types of tumor. Among all the present treatment strategies, the utmost prerequisite is prolonged intervention at the malignant site. The blood-brain barrier (BBB) is the bottleneck in the delivery of anti-GBM drugs and invasive treatment comes with many pitfalls.

Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery.

Purpose: To design and stabilize Liraglutide loaded poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) proper for oral administration.

Methods: PLGA NPs were prepared by means of double emulsion solvent evaporation method and optimized by applying 7-factor 2-level Plackett-Burman screening design.

Results: Spherical shaped NPs with homogeneous distribution, 188.

Novel strategies in the oral delivery of antidiabetic peptide drugs - Insulin, GLP 1 and its analogs.

As diabetes is a complex disorder being a major cause of mortality and morbidity in epidemic rates, continuous research has been done on new drug types and administration routes. Up to now, a large number of therapeutic peptides have been produced to treat diabetes including insulin, glucagon-like peptide-1 (GLP-1) and its analogs. The most common route of administration of these antidiabetic peptides is parenteral.