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Solubility enhancement of lawsone by complexation with beta cyclodextrin

By: Francis, Shincy Mariya.
Contributor(s): Xavier, Elizabeth N.
Publisher: Karnataka Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(3), Jul-Sep.Description: 706-715p.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian journal of pharmaceutical education and researchSummary: Introduction: Lawsone is a phyto-constituent obtained from the leaves of the Lawsonia inermis. It has antibacterial, antifungal, antiviral, wound healing, antiparasitic, tuberculostatic, anti-fertility, analgesic, anti-inflammatory, enzyme inhibitory, nematicidal, anticoagulant, and protein glycation inhibitory activities. It has poor water solubility (hydrophobic), poor bioavailability, and poor dissolution characteristics. Aim: The purpose of this research is to improve the aqueous solubility of Lawsone by preparing the inclusion complexes of Lawsone with beta-cyclodextrin. Materials and Methods: Inclusion complexes of Lawsone were prepared by different methods such as physical mixture, kneading method and co-precipitation method. Characterization of the complexes were done by Fourier Transform Infrared (FTIR) spectroscopy and in vitro dissolution study. Differential scanning calorimetry (DSC), Nuclear Magnetic Resonance spectroscopy (NMR), and Powder X-Ray Diffraction (PXRD). were used to evaluate the co-precipitation technique inclusion complexes. Antimicrobial studies of complexes against Escherichia coli (E. coli), Staphylococcus aureus (S. aureus) , Bacillus subtilis (B. subtilis), and Pseudomonas aeruginosa (P. aeruginosa ) were done by colony counting method. Results: Phase solubility study revealed the molar ratio of Lawsone to beta- cyclodextrin in the complex is 1:1. At the third hour, the drug release was 64%, 78%, 93%, and 97% for pure drug, physical mixture, inclusion complexes formed by kneading technique and co-precipitation technique respectively. DSC, NMR, and PXRD confirmed the formation of complexes of Lawsone. The order of antibacterial activity of inclusion complexes was E. coli > B. subtilis > P. aeruginosa > S. aureus.
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Introduction: Lawsone is a phyto-constituent obtained from the leaves of the
Lawsonia
inermis. It has antibacterial, antifungal, antiviral, wound healing, antiparasitic,
tuberculostatic, anti-fertility, analgesic, anti-inflammatory, enzyme inhibitory,
nematicidal, anticoagulant, and protein glycation inhibitory activities. It has poor water
solubility (hydrophobic), poor bioavailability, and poor dissolution characteristics.
Aim: The purpose of this research is to improve the aqueous solubility of Lawsone
by preparing the inclusion complexes of Lawsone with beta-cyclodextrin. Materials and
Methods: Inclusion complexes of Lawsone were prepared by different methods such as
physical mixture, kneading method and co-precipitation method. Characterization of the
complexes were done by Fourier Transform Infrared (FTIR) spectroscopy and
in vitro
dissolution study. Differential scanning calorimetry (DSC), Nuclear Magnetic Resonance
spectroscopy (NMR), and Powder X-Ray Diffraction (PXRD). were used to evaluate
the co-precipitation technique inclusion complexes. Antimicrobial studies of complexes
against
Escherichia coli
(E. coli),
Staphylococcus aureus
(S. aureus)
, Bacillus subtilis
(B. subtilis), and
Pseudomonas aeruginosa
(P. aeruginosa ) were done by colony counting
method. Results: Phase solubility study revealed the molar ratio of Lawsone to beta-
cyclodextrin in the complex is 1:1. At the third hour, the drug release was 64%, 78%,
93%, and 97% for pure drug, physical mixture, inclusion complexes formed by kneading
technique and co-precipitation technique respectively. DSC, NMR, and PXRD confirmed
the formation of complexes of Lawsone. The order of antibacterial activity of inclusion
complexes was
E. coli > B. subtilis > P. aeruginosa > S. aureus.

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