Formulation Optimization and Delivery Strategies for Self-Nanoemulsions

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 1276

Special Issue Editors


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Guest Editor
Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, NSW 2520, South Africa
Interests: self-emulsifying drug delivery systems; lipophilic drugs; lipophilic systems; natural oils; transdermal drug delivery; oral drug delivery; pseudo ternary phase diagrams; tuberculosis; malaria; tropical diseases

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Guest Editor
Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, North-West, South Africa
Interests: analytical method development; quality control of medicines; solid-state properties of pharmaceuticals; drug solubility and stability

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Guest Editor
1. FRSC, FRACI, Rural Health Research Institute, Charles Sturt University, 346 Leeds Parade, Orange, NSW 2800, Australia
2. Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, North-West, South Africa
Interests: drug development; mechanism of action of artemisinin and derivatives; combination therapy; formulation and development of drug delivery systems for topical use

Special Issue Information

Dear Colleagues,

A significant challenge in drug formulation in the pharmaceutical industry is poor aqueous solubility, a characteristic exhibited by nearly 40–60% of all newly developed drugs. The concept of self-emulsifying drug delivery systems (SEDDSs) was established during the 1960s when compounds of poor aqueous solubility were combined into mixtures with lipophilic and hydrophilic excipients to enhance their solubility. However, these thermodynamically unstable systems were only indicated in 1985 as the first tangible solution for advancing lipophilic drug delivery, and consequently bioavailability, via the oral route. Despite several decades being devoted to SEDDS and, more specifically, self-nanoemulsions, as well as their routes of delivery, pharmaceutical commercial products utilizing these delivery systems are still quite limited.

Moreover, according to the WHO, in many developing countries such as in Africa, political and economic stability is deteriorating, compromising numerous medical treatments of especially diseases of poverty that normally necessitate using lipophilic drugs. This correlation between these ailments and poverty is often a malicious cycle. Currently, poverty-related diseases are the leading cause of death in children and adolescents. They directly affect the most susceptible population, ensuing in a continued risk to global health. Furthermore, factors such as a high tablet count, poor tolerability of the drugs, and adverse effects increase non-adherence in patients. Thus, developing drug delivery systems, such as self-nanoemulsions, that are able to overcome drug absorption limitations, and that are also economically feasible, may not only meaningfully improve the subsequent bioavailability of these drugs but also enhance patient compliance and deter drug resistance.

This Special Issue is a salute to self-nanoemulsion research, embracing both fundamental and applied facets that support the present diversity of emulsions in pharmaceutical sciences and technology.

We are particularly interested in contributions in the following categories, relevant to self-nanoemulsion formulation optimization, characterization, and delivery strategies, namely:

  • Recent advances in the creation of novel self-nanoemulsion systems;
  • Self-nanoemulsion development and formulation optimization;
  • Improved quality and functionality;
  • Specialized excipients for solubilization and stabilization;
  • Characterization and stability control;
  • Emulsion rheology;
  • Drug release and bioavailability.

Dr. Joe Viljoen
Dr. Marius Brits
Prof. Dr. Richard Haynes
Guest Editors

Manuscript Submission Information

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Keywords

  • emulsions
  • self-nanoemulsifying drug delivery systems
  • formulation strategies
  • formulation optimization
  • emulsion stability
  • drug solubility
  • alternative routes of drug administration
  • drug delivery
  • drug release kinetics
  • surface active agents

Published Papers (1 paper)

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Research

22 pages, 8097 KiB  
Article
Formulation Development of Solid Self-Nanoemulsifying Drug Delivery Systems of Quetiapine Fumarate via Hot-Melt Extrusion Technology: Optimization Using Central Composite Design
by Prateek Uttreja, Ahmed Adel Ali Youssef, Indrajeet Karnik, Kavish Sanil, Nagarjuna Narala, Honghe Wang, Rasha M. Elkanayati, Sateesh Kumar Vemula and Michael A. Repka
Pharmaceutics 2024, 16(3), 324; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics16030324 - 26 Feb 2024
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Abstract
Quetiapine fumarate (QTF) was approved for the treatment of schizophrenia and acute manic episodes. QTF can also be used as an adjunctive treatment for major depressive disorders. QTF oral bioavailability is limited due to its poor aqueous solubility and pre-systemic metabolism. The objective [...] Read more.
Quetiapine fumarate (QTF) was approved for the treatment of schizophrenia and acute manic episodes. QTF can also be used as an adjunctive treatment for major depressive disorders. QTF oral bioavailability is limited due to its poor aqueous solubility and pre-systemic metabolism. The objective of the current investigation was the formulation development and manufacturing of solid self-nanoemulsifying drug delivery system (S-SNEDDS) formulation through a single-step continuous hot-melt extrusion (HME) process to address these drawbacks. In this study, Capmul® MCM, Gelucire® 48/16, and propylene glycol were selected as oil, surfactant, and co-surfactant, respectively, for the preparation of S-SNEDDS. Soluplus® and Klucel™ EF (1:1) were selected as the solid carrier. Response surface methodology in the form of central composite design (CCD) was utilized in the current experimental design to develop the S-SNEDDS formulations via a continuous HME technology. The developed formulations were evaluated for self-emulsifying properties, particle size distribution, thermal behavior, crystallinity, morphology, physicochemical incompatibility, accelerated stability, and in vitro drug release studies. The globule size and emulsification time of the optimized SNEDDS formulation was 92.27 ± 3.4 nm and 3.4 ± 3.38 min. The differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies revealed the amorphous nature of the drug within the formulation. There were no drug-excipient incompatibilities observed following the Fourier transform infrared (FTIR) spectroscopy. The optimized formulation showed an extended-release profile for 24 h. The optimized formulation was stable for three months (last time-point tested) at 40 °C/75% RH. Therefore, the developed S-SNEDDS formulation could be an effective oral delivery platform for QTF and could lead to better therapeutic outcomes. Full article
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