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'Poly phenolic phytoceutical loaded nano-bilosomes for enhanced caco-2 cell permeability and SARS-CoV 2 antiviral activity': in-vitro and insilico studies.
Zakaria, Mohamed Y; Abd El-Halim, Shady M; Beshay, Botros Y; Zaki, Islam; Abourehab, Mohammed A S.
  • Zakaria MY; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Port Said University, Port Said, Egypt.
  • Abd El-Halim SM; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Salman International University (KSIU), South Sinai, Ras Sudr, Egypt.
  • Beshay BY; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, 6th of October City, Giza, Egypt.
  • Zaki I; Pharmaceutical Sciences (Pharmaceutical Chemistry) Department, College of Pharmacy, Arab Academy for Science, Technology and Maritime Transport, Alexandria, Egypt.
  • Abourehab MAS; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, Egypt.
Drug Deliv ; 30(1): 2162157, 2023 Dec.
Article in English | MEDLINE | ID: covidwho-2166083
ABSTRACT
Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) predisposed to the emergence of worldwide catastrophe that impels the evolution of safe and effective therapeutic system. Polyphenols as resveratrol (RSV) exhibit a well evidenced antiviral activity. Unfortunately, like most phenolic nutraceuticals, RSV suffers from restrained solubility and massive degradation in GIT and liver which in turn prohibit its clinical use. Herein, PEGylated bilosomes (PBs) contain PEGylated edge activator along with the traditional components as (Span 60, cholesterol and bile salts) were proposed to boost both permeability and bioavailability of RSV. The investigation of the prominent effect of the diverse variables on the characteristics of the vesicles and picking of the optimum formula were conducted via construction of 23 factorial experiment. The appraisal of the formulae was conducted on the basis of entrapment efficiency percent (EE%), particle size (PS) and zeta potential (ZP). In addition, the spherical shaped optimal formula (F5) exhibited EE% of 86.1 ± 2.9%, PS of 228.9 ± 8.5 nm, and ZP of -39.8 ± 1.3 mV. The sorted optimum formula (F5) exhibited superior dissolution behaviors, and boosted Caco-2 cells cellular uptake by a round 4.7 folds relative to RSV dispersion. In addition, F5 demonstrated a complete in vitro suppression of SARS-CoV-2 at a concentration 0.48 µg/ml with 6.6 times enhancement in antiviral activity relative to RSV dispersion. The accomplished molecular modeling heavily provided proof for the possible interactions of resveratrol with the key residues of the SARS-CoV2 Mpro enzyme. Finally, F5 could be proposed as a promising oral panel of RSV for curation from SARS-CoV-2 infection.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: SARS-CoV-2 / COVID-19 Type of study: Prognostic study / Randomized controlled trials Limits: Humans Language: English Journal: Drug Deliv Journal subject: Pharmacology / Drug Therapy Year: 2023 Document Type: Article Affiliation country: 10717544.2022.2162157

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Full text: Available Collection: International databases Database: MEDLINE Main subject: SARS-CoV-2 / COVID-19 Type of study: Prognostic study / Randomized controlled trials Limits: Humans Language: English Journal: Drug Deliv Journal subject: Pharmacology / Drug Therapy Year: 2023 Document Type: Article Affiliation country: 10717544.2022.2162157