Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization

Topic Information

Dear Colleagues,

This theme aims to explore the diverse world of drug delivery systems, emphasising the integration of various techniques and approaches to enhance drug efficacy, stability, and patient compliance. It will cover a range of topics, including but not limited to, the following:

• Advancements in Spray Drying: Focusing on novel techniques using two- and multiple-fluid spray drying to improve drug solubility and bioavailability, particularly for poorly soluble drugs;
• Innovations in Inhalation Drug Delivery: Highlighting the latest developments in pulmonary drug delivery systems, with a special focus on patient compliance and the role of particle engineering in enhancing drug efficacy;
• Crystal Engineering in Pharmaceuticals: Discussing the impact of crystal engineering on drug properties, such as solubility, stability, and bioavailability, and its role in overcoming formulation challenges;
• Emerging Trends in Oral Drug Delivery: Exploring new technologies and approaches in oral drug delivery, including targeted delivery systems and strategies to overcome biological barriers for improved drug absorption;
• Cross-Disciplinary Approaches: Encouraging submissions that demonstrate the intersection of these areas, such as the use of crystal engineering in inhalation drug delivery or the application of two- and three-fluid spray drying techniques in oral drug formulations.

Prof. Dr. Barbara R. Conway
Dr. Hisham Al-Obaidi
Topic Editors

Keywords

Participating Journals

Journal Name	Impact Factor	CiteScore	Launched Year	First Decision (median)	APC
Bioengineering bioengineering	3.7	5.3	2014	19.2 Days	CHF 2700	Submit
Molecules molecules	4.6	8.6	1996	16.1 Days	CHF 2700	Submit
Pharmaceuticals pharmaceuticals	4.8	7.7	2004	14 Days	CHF 2900	Submit
Pharmaceutics pharmaceutics	5.5	10.0	2009	14.9 Days	CHF 2900	Submit
Processes processes	2.8	5.5	2013	16 Days	CHF 2400	Submit
Scientia Pharmaceutica scipharm	2.5	4.6	1930	38.1 Days	CHF 1000	Submit

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Published Papers (5 papers)

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All Bioengineering Molecules Pharmaceuticals Pharmaceutics Processes Sci. Pharm.

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46 pages, 3987 KB  

Open AccessReview

Niosomes as Vesicular Carriers: From Formulation Strategies to Stimuli-Responsive Innovative Modulations for Targeted Drug Delivery

by Andra Ababei-Bobu, Bianca-Ștefania Profire, Andreea-Teodora Iacob, Oana-Maria Chirliu, Florentina Geanina Lupașcu and Lenuța Profire

Pharmaceutics 2025, 17(11), 1473; https://doi.org/10.3390/pharmaceutics17111473 - 14 Nov 2025

Viewed by 623

Abstract

Niosomes (NIOs), a class of nanovesicular drug delivery system, have garnered significant attention due to their unique architecture, resulting from the self-assembly of non-ionic surfactants (with or without cholesterol) in aqueous media. This bilayered structure enables the encapsulation of both hydrophilic agents in [...] Read more.

Niosomes (NIOs), a class of nanovesicular drug delivery system, have garnered significant attention due to their unique architecture, resulting from the self-assembly of non-ionic surfactants (with or without cholesterol) in aqueous media. This bilayered structure enables the encapsulation of both hydrophilic agents in the aqueous core and lipophilic compounds within the lipid bilayer, offering remarkable versatility in therapeutic applications. This article provides an overview of the key principles underlying niosomal formulations, including their composition, preparation methods, formulation conditions and the critical physicochemical parameters influencing vesicle formation and performance. Special emphasis is placed on recent innovations in surface and content modifications that have led to the development of stimuli-responsive niosomal systems, with precise and controlled drug release. These smart carriers are designed to respond to endogenous stimuli (such as pH variations, redox gradients, enzymatic activity, or local temperature changes in pathological sites), as well as to exogenous triggers (including light, ultrasound, magnetic or electric fields, and externally applied hyperthermia), thereby enhancing therapeutic precision. These surface and content modulation strategies effectively transform conventional NIOs into intelligent, stimuli-responsive platforms, reinforcing their innovative role in drug delivery and highlighting their significant potential in the development of smart nanomedicine. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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18 pages, 1936 KB  

Open AccessArticle

Does a Polycistronic 2A Design Enable Functional FcRn Production for Antibody Pharmacokinetic Studies?

by Valentina S. Nesmeyanova, Nikita D. Ushkalenko, Sergei E. Olkin, Maksim N. Kosenko, Elena A. Rukhlova, Ivan M. Susloparov and Dmitry N. Shcherbakov

Pharmaceutics 2025, 17(11), 1463; https://doi.org/10.3390/pharmaceutics17111463 - 13 Nov 2025

Viewed by 440

Abstract

Background/Objectives: The neonatal Fc receptor (FcRn) is a heterodimeric protein composed of a heavy α-chain with an MHC class I-like fold and β₂-microglobulin. It plays a crucial role in maintaining the homeostasis and pharmacokinetics of immunoglobulin G (IgG) and albumin through [...] Read more.

Background/Objectives: The neonatal Fc receptor (FcRn) is a heterodimeric protein composed of a heavy α-chain with an MHC class I-like fold and β₂-microglobulin. It plays a crucial role in maintaining the homeostasis and pharmacokinetics of immunoglobulin G (IgG) and albumin through pH-dependent recycling. The production of soluble recombinant FcRn is technically challenging due to its heterodimeric structure and the presence of a transmembrane domain. This study aimed to develop a polycistronic construct enabling the co-expression of FcRn subunits from a single transcript and to evaluate the functional activity of the resulting protein in CHO-K1 cells. Methods: Integration vectors (pComV-FcRn-B2M) were designed to encode FcRn and β₂-microglobulin linked via self-cleaving 2A peptides (P2A, E2A, F2A, T2A). Stable producer cell lines were generated using the Sleeping Beauty transposon system. The purified proteins were characterized by SDS-PAGE, Western blotting, and size-exclusion chromatography (SEC). Functional activity was assessed by ELISA and bio-layer interferometry (BLI). Results: Electrophoretic and chromatographic analyses confirmed the expected subunit composition and demonstrated that over 95% of the recombinant protein was monomeric. Functional assays revealed pH-dependent IgG binding, with strong interaction at pH 6.0 and negligible binding at pH 7.5. BLI measurements showed high affinity consistent with native FcRn function (KD = 3.15 nM at pH 6.0). Conclusions: The developed polycistronic construct containing a P2A peptide with a GSG linker enabled efficient production of functional FcRn in CHO-K1 cells (yield up to 2.23 mg/mL). The P2A variant demonstrated the highest efficiency and can serve as a reference system for screening Fc-engineered antibodies with optimized pharmacokinetic properties. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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17 pages, 2110 KB  

Open AccessEditor’s ChoiceArticle

5-Aminosalicylic Acid Distribution into the Intestinal Membrane Along the Gastrointestinal Tract After Oral Administration in Rats

by Yorinobu Maeda, Yuta Goto, Fumiya Ohnishi, Syoutarou Koga, Satoshi Kawano, Yuhzo Hieda, Takeshi Goromaru and Teruo Murakami

Pharmaceutics 2024, 16(12), 1567; https://doi.org/10.3390/pharmaceutics16121567 - 7 Dec 2024

Cited by 3 | Viewed by 1993

Abstract

Background: 5-Aminosalicylic acid (5-ASA), the first-line therapy for ulcerative colitis, is a poorly soluble zwitterionic drug. Unformulated 5-ASA is thought to be extensively absorbed in the small intestine. Methods: The pH-dependent solubility of 5-ASA in vitro and the intestinal membrane distribution of 5-ASA [...] Read more.

Background: 5-Aminosalicylic acid (5-ASA), the first-line therapy for ulcerative colitis, is a poorly soluble zwitterionic drug. Unformulated 5-ASA is thought to be extensively absorbed in the small intestine. Methods: The pH-dependent solubility of 5-ASA in vitro and the intestinal membrane distribution of 5-ASA and its N-acetyl metabolite (AC-5-ASA) after the oral administration of 5-ASA were examined in fed rats. 5-ASA was administered as a suspension in water, 0.1 M HCl, or 0.1 M NaOH to untreated rats or as a solution in 5% NaHCO₃ to lansoprazole-pretreated rats. Results: 5-ASA solubility in vitro was higher at pH < 2 and pH > 7. In rats, the 5-ASA and AC-5-ASA were detected mostly in the small intestine at 3 h and in the colonic region at 8 h after administration. The dosing vehicle (suspension or solution) and lansoprazole pretreatment did not significantly affect the pH of the luminal fluid in rats or the 5-ASA distribution in membranes. Conclusions: The 5-ASA distribution in membranes in the proximal intestine was found to be restricted by the intrinsic regional luminal pH, low solubility, and saturable membrane permeability. Unabsorbed 5-ASA in the proximal intestine was delivered to the distal intestine. The higher the oral dose of 5-ASA, the more 5-ASA may be delivered to the distal intestine due to the restricted absorption in the small intestine. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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25 pages, 4244 KB  

Open AccessArticle

Back to Nature: Development and Optimization of Bioinspired Nanocarriers for Potential Breast Cancer Treatment

by Sally Safwat, Rania M. Hathout, Rania A. H. Ishak and Nahed D. Mortada

Sci. Pharm. 2024, 92(3), 50; https://doi.org/10.3390/scipharm92030050 - 2 Sep 2024

Viewed by 2736

Abstract

This study focuses on the preparation and optimization of caffeic acid (CA)-loaded casein nanoparticles (CS NPs) via the Box–Behnken design (BBD) for potential applications in cancer treatment. CS NPs were loaded with CA as a promising anti-cancer molecule. Non-hazardous green materials were exploited [...] Read more.

This study focuses on the preparation and optimization of caffeic acid (CA)-loaded casein nanoparticles (CS NPs) via the Box–Behnken design (BBD) for potential applications in cancer treatment. CS NPs were loaded with CA as a promising anti-cancer molecule. Non-hazardous green materials were exploited for nanoparticle fabrication. The BBD was used, followed by a desirability function to select the optimum formulation. The BBD was adopted as it avoids the runs implemented in extreme conditions, hence making it suitable for proteins. CS NPs were characterized regarding particle size (PS), size distribution (PDI), zeta potential (ZP), drug entrapment, morphology using TEM, differential scanning calorimetry, molecular docking, in vitro release, and cytotoxicity studies. PS, PDI, and ZP had significant responses, while EE% was insignificant. The suggested models were quadratic with high fitting. Optimized NPs showed PS = 110.31 ± 1.02 nm, PDI = 0.331 ± 0.029, ZP = −23.94 ± 1.64 mV, and EE% = 95.4 ± 2.56%. Molecular modeling indicated hydrophobic and electrostatic interactions between CA and CS, accounting for the high EE%. Almost spherical particles were realized with a sustained CA release pattern. Optimized NPs effectively suppressed the growth of MCF-7 cell lines by scoring the lowest IC50 = 78.45 ± 1.7 µg/mL. A novel combination of bioinspired-derived materials was developed for use in breast cancer treatment. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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20 pages, 2334 KB  

Open AccessArticle

Phosal^® Curcumin-Loaded Nanoemulsions: Effect of Surfactant Concentration on Critical Physicochemical Properties

by Joanna Czerniel, Aleksandra Gostyńska, Tomasz Przybylski and Maciej Stawny

Sci. Pharm. 2024, 92(3), 48; https://doi.org/10.3390/scipharm92030048 - 30 Aug 2024

Cited by 3 | Viewed by 3250

Abstract

Curcumin is a well-known and widely used substance of natural origin. It has also been found to be helpful in the treatment of liver diseases. Unfortunately, curcumin has very low bioavailability and a sensitivity to external agents. Improving these parameters is the subject [...] Read more.

Curcumin is a well-known and widely used substance of natural origin. It has also been found to be helpful in the treatment of liver diseases. Unfortunately, curcumin has very low bioavailability and a sensitivity to external agents. Improving these parameters is the subject of many studies. One way to overcome these problems may be to use Phosal^® Curcumin as a source of curcumin and encapsulate this dispersion into a nanoemulsion using different types and concentrations of surfactants and co-surfactants, thus manipulating the physicochemical parameters of the nanoemulsion. The present study aimed to develop curcumin-loaded nanoemulsions for intravenous administration and to investigate the effect of Kolliphor HS15 concentration on their critical quality attributes. Methods: Phosal^® Curcumin-loaded nanoemulsions with different concentrations of Kolliphor HS15 were prepared by high-pressure homogenization. The effect of Kolliphor HS15 on emulsion physicochemical properties such as mean droplet diameter (MDD), polydispersity index (PDI), zeta potential (ZP), osmolality (OSM), and pH, as well as encapsulation efficiency (EE) and retention rate (RR) of curcumin, were determined. Mid-term stability studies and short-term stress tests were conducted to evaluate the impact of Kolliphor HS15 on the critical quality attributes of the curcumin-loaded nanoemulsions stored under various conditions. Results: Five nanoemulsions with increasing Kolliphor HS15 concentrations were developed. Their MDD ranged from 85.2 ± 2.0 to 154.5 ± 5.1 nm, with a PDI from 0.18 ± 0.04 to 0.10 ± 0.01 and ZP from −15.6 ± 0.7 to −27.6 ± 3.4 mV. Depending on the concentration of Kolliphor HS15, the EE ranged from 58.42 ± 1.27 to 44.98 ± 0.97%. Conclusions: The studied parameters of the developed nanoemulsions meet the requirements for formulations for intravenous administration. Using the appropriate concentration of Kolliphor HS15 allows for a formulation that presents a protective effect against both curcumin and emulsion degradation. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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