Natural Bioactive Substances: Microencapsulation Technologies, Pharmacological Efficacies and Sustainable Application in Pharmaceuticals

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: 25 May 2026 | Viewed by 1796

Special Issue Editors


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Guest Editor
Department of Drug Technology and Social Pharmacy, Faculty of Pharmacy, Medical Academy, Lithuanian University of Health Sciences, Sukileliu pr. 13, LT-50161 Kaunas, Lithuania
Interests: natural ingredients; pharmaceutical forms; microencapsulation; 3D printing
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Guest Editor
Instrumental Analysis Open Access Center, Faculty of Natural Sciences, Vytautas Magnus University, Kaunas, Lithuania
Interests: analytical chemistry; development of separation methods; capillary electrophoresis; coupling and miniaturization of methods; food analysis; fermentation; biotechnology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural bioactive substances (NBS), derived from plants, animals, microorganisms and marine organisms, possess diverse pharmacological properties such as anti-inflammatory, antioxidant, antitumor, and neuroprotective effects, making them promising candidates for pharmaceutical development. However, their clinical application is often limited by inherent drawbacks: poor water solubility, low stability (susceptible to heat, light, and enzymatic degradation), short in vivo half-life, and low bioavailability. Microencapsulation technologies—including spray drying, electrostatic spinning, liposome encapsulation, alginate-based hydrogel encapsulation, and coacervation—have emerged as effective solutions to address these challenges. By enclosing NBS in biocompatible and biodegradable carriers (e.g., lipids, polysaccharides and proteins), microencapsulation not only enhances the solubility and stability of NBS but also enables controlled/sustained drug release, targeted delivery to specific tissues or organs, and a reduction in potential side effects, thereby significantly improving their pharmacological efficacy and therapeutic safety.

This Special Issue of Pharmaceuticals aims to gather cutting-edge research, reviews, and technical reports focusing on microencapsulation technologies for NBS, their pharmacological efficacy evaluation, and sustainable pharmaceutical applications. We welcome contributions covering, but not limited to, the following areas: (1) Innovation and optimization of microencapsulation technologies for NBS (e.g., novel carrier materials, improved preparation processes); (2) In vitro/in vivo evaluation of the pharmacological efficacy, bioavailability, and safety of microencapsulated NBS; (3) Mechanistic studies on how microencapsulation enhances the stability, solubility, and targeting of NBS; (4) Development of sustainable extraction, purification, and microencapsulation processes for NBS; (5) Design and application of microencapsulated NBS in pharmaceutical formulations (e.g., oral preparations, injectables, topical formulations); and (6) Case studies on the clinical translation of microencapsulated NBS-based pharmaceutical products.

By compiling these studies, this Special Issue will systematically summarize the latest progress in the field of NBS microencapsulation and sustainable pharmaceutical application, deepen the understanding of the synergy between microencapsulation technologies and NBS pharmacological properties, and provide theoretical and technical support for promoting the development of green, efficient, and clinically applicable NBS-based pharmaceuticals.

Dr. Lauryna Pudžiuvelytė
Dr. Mantas Stankevičius
Guest Editors

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Keywords

  • natural bioactive substances
  • microencapsulation technologies
  • pharmacological efficacy
  • sustainable pharmaceutical application
  • drug carrier materials
  • bioavailability
  • controlled release
  • green pharmacy

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Published Papers (2 papers)

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Research

25 pages, 2566 KB  
Article
Development of Phyllanthus emblica Extract-Loaded Niosomes for Cancer Treatment: Formulation and In Vitro Evaluation
by Al-Zahraa Khalifa, Naglaa Gamil Shehab, Dema Layth Jabbar, Heba Marwan Ibrahim, Manar Ahmed Hawash, Maryam Jamal Afif Said, Aliasgar Shahiwala and Bazigha K. Abdul Rasool
Pharmaceuticals 2026, 19(4), 582; https://doi.org/10.3390/ph19040582 - 6 Apr 2026
Viewed by 673
Abstract
Phyllanthus emblica (amla) exhibits anticancer activity, but its extracts often suffer from poor stability and bioavailability. This study developed amla extract-loaded niosomes to enhance delivery and evaluate their anticancer activity against MCF-7 and HCT116 cell lines, supported by in silico analyses. Methodology: Amla [...] Read more.
Phyllanthus emblica (amla) exhibits anticancer activity, but its extracts often suffer from poor stability and bioavailability. This study developed amla extract-loaded niosomes to enhance delivery and evaluate their anticancer activity against MCF-7 and HCT116 cell lines, supported by in silico analyses. Methodology: Amla extract was prepared using a 50% aqueous–alcoholic solvent system and lyophilized. Niosomes were prepared by the thin-film hydration method and characterized for physicochemical properties. Anticancer activity was evaluated through in vitro cytotoxicity studies, supported by molecular docking and in silico pharmacokinetic analyses. Results: Optimized niosomes exhibited spherical morphology, good homogeneity (PDI < 0.30), anionic surface charge, high entrapment efficiency (70.5 ± 5.9%), and sustained diffusion-controlled release. In vitro cytotoxicity demonstrated a strong concentration-dependent anticancer activity of amla-loaded niosomes across a range of concentrations (31.25–1000 µg/mL) against both MCF-7 and HCT116 cell lines. At 1000 µg/mL, cell viability decreased to 7.0% and 5.4% in MCF-7 and HCT116 cells, respectively, with calculated IC50 values of 245 µg/mL and 158 µg/mL. Molecular docking and pharmacokinetic predictions supported the potential multi-target anticancer relevance of major phytochemicals, including hydrolyzable tannins, phenolic acids, flavonoid aglycones and glycosides, and highlighted bioavailability limitations for certain high-affinity glycosylated flavonoids, reinforcing the rationale for vesicular encapsulation. Conclusions: Amla extract-loaded niosomes represent a promising vesicular system for enhanced, sustained delivery of anticancer activity in vitro, with complementary in silico findings supporting mechanistic plausibility and translational rationale. Further studies are warranted to evaluate their performance in vivo. Full article
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20 pages, 3047 KB  
Article
From Berries to Capsules: Technological and Quality Aspects of Juneberry Formulations
by Lauryna Pudžiuvelytė and Agnė Mačiulskaitė
Pharmaceuticals 2025, 18(12), 1841; https://doi.org/10.3390/ph18121841 - 2 Dec 2025
Cited by 2 | Viewed by 784
Abstract
Background: Amelanchier alnifolia (Juneberry) is a phenolic-rich species with potential for pharmaceutical applications. This study aimed to optimize ultrasound-assisted extraction (UAE) conditions for producing ethanolic extracts from differently processed Juneberry berries collected in Lithuania and to develop solid oral dosage forms based [...] Read more.
Background: Amelanchier alnifolia (Juneberry) is a phenolic-rich species with potential for pharmaceutical applications. This study aimed to optimize ultrasound-assisted extraction (UAE) conditions for producing ethanolic extracts from differently processed Juneberry berries collected in Lithuania and to develop solid oral dosage forms based on the obtained extracts. Methods: Extracts were prepared using varying ethanol concentrations, temperatures, and extraction times from dried, frozen, and freeze-dried berries. Total phenolic content (TPC) and total flavonoid content (TFC) were determined spectrophotometrically. Antioxidant activity was evaluated by DPPH and ABTS assays. Phenolic profiles were quantified by high-performance liquid chromatography (HPLC), identifying five major compounds. Extracts were converted into powders using lactose monohydrate, microcrystalline cellulose, or magnesium aluminum metasilicate as carriers. Hard capsules were manufactured and evaluated according to European Pharmacopoeia (Ph. Eur.) requirements, including mass uniformity, moisture content, and disintegration time. Results: Freeze-dried berries yielded the highest TPC, TFC, and antioxidant activity across all extraction conditions. The most efficient extraction parameters for freeze-dried berries were identified as 50% ethanol, 50–55 °C, and 30 min. HPLC analysis confirmed the presence of chlorogenic and neochlorogenic acids, rutin, hyperoside, and isoquercitrin. Among the powdered systems, lactose monohydrate demonstrated favorable flowability and moisture characteristics. Conclusions: Freeze-dried Juneberry berries are a suitable raw material for producing phenolic-rich extracts with strong antioxidant activity. Lactose-based powder blends showed the best technological performance and were successfully formulated into hard capsules. These findings support the potential of Juneberry extracts for incorporation into standardized pharmaceutical dosage forms and provide a basis for future formulation and bioavailability studies. Full article
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