Enhancing Dissolution Rate and Antibacterial Efficiency of Azithromycin through Drug-Drug Cocrystals with Paracetamol

Islam, Noor; Khan, Ezzat; Umar, Muhammad Naveed; Shah, Attaullah; Zahoor, Muhammad; Ullah, Riaz; Bari, Ahmed

doi:10.3390/antibiotics10080939

Cited by 18 publications

(9 citation statements)

References 74 publications

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“…The improvement of antibacterial activity against bacterial strains through cocrystallization [ 8 , 20 , 83 , 84 , 85 ] and amorphous salt [ 19 ] has been reported in literature. Therefore, the comparative zone of inhibition and minimum inhibitory concentration (MIC) studies of LEV and respective formulations were performed against bacterial strains Escherichia coli ( E. coli ), MTCC 1687; Salmonella typhi ( S. typhi ), MTCC 734 and Klebsiella pneumonia ( K. pneumonia ), MTCC 1030; the results have been presented in Table 2 and Table 3 .…”

Section: Resultsmentioning

confidence: 99%

“…Such multicomponent solid formulations containing an API and a coformer in a well-defined stoichiometric ratio and interact through non-covalent interactions. Cocrystallization [ 8 , 9 ], designing of salt [ 10 , 11 , 12 ] and coamorphization [ 5 , 6 , 7 ] approaches are preferably used to enhance the solubility, dissolution rate and permeability. Recently such approaches have been used for taste masking [ 13 , 14 ], photostabilization [ 15 , 16 , 17 ], color tuning [ 18 ] and improving antimicrobial properties [ 8 , 12 , 19 , 20 ].…”

Section: Introductionmentioning

confidence: 99%

“…Cocrystallization [ 8 , 9 ], designing of salt [ 10 , 11 , 12 ] and coamorphization [ 5 , 6 , 7 ] approaches are preferably used to enhance the solubility, dissolution rate and permeability. Recently such approaches have been used for taste masking [ 13 , 14 ], photostabilization [ 15 , 16 , 17 ], color tuning [ 18 ] and improving antimicrobial properties [ 8 , 12 , 19 , 20 ]. Cocrystals/salts of ciprofloxacin with thymol, carvacrol [ 20 ], hippurate [ 12 ] and polymers [ 19 ] have been successfully prepared.…”

Section: Introductionmentioning

confidence: 99%

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Levofloxacin Cocrystal/Salt with Phthalimide and Caffeic Acid as Promising Solid-State Approach to Improve Antimicrobial Efficiency

et al. 2022

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To overcome the issue of multidrug resistant (MDR) microbes, the exploration of ways to improve the antimicrobial efficiency of existing antibiotics is one of the promising approaches. In search of synthons with higher efficiency, in current investigations, cocrystal and amorphous salt of levofloxacin hemihydrate (LEV) were developed with phthalimide (PTH) and caffeic acid (CFA). New materials were characterized with the help of FT-IR, Raman spectroscopy, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). Shifting, attenuation, appearance/disappearance and broadening of bands were observed in the FT-IR and Raman spectra of the materials as evidence of the required product. The PXRD diffraction pattern observed for LEV-PTH indicated cocrystal while halo diffractogram of LEV-CFA revealed amorphous nature. DSC/TG analysis confirmed the hydrated nature of the cocrystal/salt. The dissolution rate and antimicrobial activity against selected strains, K.pneumonia, E. coli and S. typhi of parent drug and the new material were compared. The zone of inhibition (ZI) observed for 5 µg LEV-PTH was 30.4 + 0.36 (K. pneumonia), 26.33 + 0.35 (E. coli) and 30.03 + 0.25 mm (S. typhi) while LEV-CFA salt (5 µg) against the same strains inhibited 33.96 ± 0.25, 31.66 ± 0.35 and 27.93 ± 0.40 mm, respectively. These novel formulations enhance the dissolution rate as well as antibacterial efficiency and are expected to be potent against MDR bacterial strains.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Levofloxacin Cocrystal/Salt with Phthalimide and Caffeic Acid as Promising Solid-State Approach to Improve Antimicrobial Efficiency

et al. 2022

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“…Combination therapy allows the use of lower concentrations and therefore minimizes the advent of probable toxicity [ 26 , 27 ]. The type of interaction that results from the combination of colistin and orientin against both K. pneumoniae and P. aeruginosa was synergistic as the FICI was 0.37 and 0.31, respectively.…”

Section: Discussionmentioning

confidence: 99%

Orientin Enhances Colistin-Mediated Bacterial Lethality through Oxidative Stress Involvement

Khumbulani

Alayande

Sabiu

2022

Evidence-Based Complementary and Alternative Medicine

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Bacterial resistance to colistin has prompted the search for alternative strategies to enhance antibacterial potential. Combination therapy remains one of the viable strategies in antibacterial therapy and has been proven to be effective in reducing the risk of resistance. In this study, the potential of orientin for enhancing the antibacterial activity of colistin was assessed against Klebsiella pneumoniae and Pseudomonas aeruginosa in vitro. The involvement of oxidative stress in such enhancement was also assessed. The minimum inhibitory concentrations (MICs) of colistin and orientin were 16 μg/mL and 64 μg/mL against K. pneumoniae and 64 μg/mL and 256 μg/mL against P. aeruginosa respectively. For the combination therapy, orientin potentiates the antibacterial effect of colistin with a friction inhibitory concentration index (FICI) of 0.37 and 0.31 against K. pneumoniae and P. aeruginosa, respectively. This observation suggests a synergistic interaction, with the MIC of colistin being reduced by 3- and 4-fold in the presence of orientin against K. pneumoniae and P. aeruginosa, respectively. Additionally, treatment with the combination of colistin and orientin induced oxidative stress against both organisms through increased cellular levels of superoxide anion radicals with concomitant increase in NAD+/NADH and ADP/ATP ratios. These findings suggest that orientin enhanced colistin in the killing of the test bacteria and the cotreatment of colistin and orientin induced oxidative stress, through reactive oxygen species generation, which consequently facilitated bacterial lethality without causing drug-drug interactions. Although, the data presented in this study has supported the capability of orientin for strengthening antibacterial activity of colistin toward the fight against drug-resistant Gram-negative bacteria, studies focusing on the exact target and mechanism of action of orientin are underway.

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“…• Electrostatic repulsion: [12] The interaction of the electrical double layers around the charged droplets produces electrostatic force, which tends to avoid droplet contact. An ionic surfactant is adsorbed to cause this process.…”

Section: Mechanisms Of Emulsion Stabilization:[12]mentioning

confidence: 99%

Review on: Preparation and Evaluation of Paracetamol Emulsion dosage Form

Kumar¹,

Parveen²

2022

J. Res. Appl. Sci. Biotechnol.

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The objective of this review article is to summarize literature data pertinent to potential excipient effects on intestinal drug permeability and transit. Despite the use of excipients in drug products for decades, considerable research efforts have been directed towards evaluating their potential effects on drug bioavailability. Potential excipient concerns stem from drug formulation changes (e.g., scale-up and post-approval changes, development of a new generic product). Regulatory agencies have established in vivo bioequivalence standards and, as a result, may waive the in vivo requirement, known as a biowaiver, for some oral products. Biowaiver acceptance criteria are based on the in vitro characterization of the drug substance and drug product using the Biopharmaceutics Classification System (BCS). Various regulatory guidance documents have been issued regarding BCS-based biowaivers, such that the current FDA guidance is more restrictive than prior guidance, specifically about excipient risk. In particular, sugar alcohols have been identified as potential absorption-modifying excipients. These biowaivers and excipient risks are discussed here.

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Enhancing Dissolution Rate and Antibacterial Efficiency of Azithromycin through Drug-Drug Cocrystals with Paracetamol

Cited by 18 publications

References 74 publications

Levofloxacin Cocrystal/Salt with Phthalimide and Caffeic Acid as Promising Solid-State Approach to Improve Antimicrobial Efficiency

Levofloxacin Cocrystal/Salt with Phthalimide and Caffeic Acid as Promising Solid-State Approach to Improve Antimicrobial Efficiency

Orientin Enhances Colistin-Mediated Bacterial Lethality through Oxidative Stress Involvement

Review on: Preparation and Evaluation of Paracetamol Emulsion dosage Form

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