Phytotherapeutics self-microemulsifying systems in pellet dosage form for enhanced intestinal drug delivery: formulation, stability, and in-vivo performance
PUBMED · rheumatology · EN
Shrnutí pro lékaře
1. Drug Deliv. 2026 Dec 31;33(1):2702133. doi: 10.1080/10717544.2026.2702133. Epub 2026 Jul 15. Phytotherapeutics self-microemulsifying systems in pellet dosage form for enhanced intestinal drug delivery: formulation, stability, and in-vivo performance. Koutná G(1), Kotouček J(2), Macků J(1), Kubová K(1), Urbanová M(3), Janisová L(3), Šeděnková I(3), Muselík J(1), Vysloužil J(1), Mašek J(2), Mašková E(2), Pavelková M(1), Vetchý D(1), Brus J(3). Author information: (1)Department of Pharma
Shrnutí pro pacienty
1. Drug Deliv. 2026 Dec 31;33(1):2702133. doi: 10.1080/10717544.2026.2702133.
Epub 2026 Jul 15.
Phytotherapeutics self-microemulsifying systems in pellet dosage form for
enhanced intestinal drug delivery: formulation, stability, and in-vivo
performance.
Koutná G(1), Kotouček J(2), Macků J(1), Kubová K(1), Urbanová M(3), Janisová
L(3), Šeděnková I(3), Muselík J(1), Vysloužil J(1), Mašek J(2), Mašková E(2),
Pavelková M(1), Vetchý D(1), Brus J(3).
Author information:
(1)Department of Pharmaceutical Technology, Faculty of Pharmacy, Masaryk
University Brno, Brno, Czech Republic.
(2)Department of Pharmacology and Toxicology, Veterinary Research Institute,
Brno, Czech Republic.
(3)Department of Structural Analysis, Institute of Macromolecular Chemistry,
Czech Academy of Sciences, Praque, Czech Republic.
Self-microemulsifying drug delivery systems (SMEDDS) containing volatile
phytotherapeutics such as thymol (T), carvacrol (C), and eugenol (E) present
significant formulation challenges, even when solidified. Their instability and
interactions with coatings often hinder intestinal delivery. To address these
limitations, we developed solid SMEDDS consisting of pellets (microcrystalline
cellulose/magnesium aluminometasilicate/chitosan) and enteric capsules (CEC) for
enhanced intestinal delivery. Based on solubility and pseudo-ternary phase
diagrams, SMEDDS formulations (SES1-3) differing in component ratios (glycerol
monooleate/caprylocaproyl macrogol-8 glycerides/diethylene glycol monoethyl
ether) with 5% w/w of each drug were identified, demonstrating nano-scale
droplet sizes (PDI <0.4) and showing no phase separation over 6 months.
Thermodynamic stability and liquid-state NMR revealed particle size variations
with preserved structural integrity. The lead formulation SES1 exhibited
superior ex-vivo intestinal permeation (T-SES1). CECs filled with T-, C-, and
E-loaded SES1 pellets, respectively, prepared via extrusion/spheronization,
exhibited in-vitro gastro-resistant release, and achieved > 85% drug release
within 120 min after a pH change to 6.8 during a one-year stability study
(25 °C; 60% RH). FTIR-ATR analysis of the CEC internal surface confirmed the
temperature-dependent restructuring of hypromellose and E sorption, a phenomenon
not observed with C or T, which is likely attributable to physicochemical
distinctions. Oral administration of CEC with T-SES1-pellets (0.5 mg/kg) in
piglets demonstrated a delayed peak plasma concentration (Cmax 11.67 ng/mL at
9 h) and sustained systemic exposure (AUC 119.8 ng·h/mL). These in-vivo findings
substantiate the gastro-protective effect and enhanced intestinal absorption,
positioning the pellet/CEC system as a promising strategy for the application of
volatile phytotherapeutics in current pharmacotherapy.
DOI: 10.1080/10717544.2026.2702133
PMID: 42454740 [Indexed for MEDLINE]
Původní zdroj →AI kategorie
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"specialty": "rheumatology",
"study_type": "cohort",
"evidence_level": "level-3",
"v6_autopublish": true,
"clinical_impact": "moderate-impact",
"practice_recommendation": "monitoring"
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