Cyclodextrin Derivative Enhances the Ophthalmic Delivery of Poorly Soluble Azithromycin

Thakur, Anil; Jain, Sourabh; Pant, Anjali; Sharma, Akanksha; Kumar, Rajiv; Singla, Neha; Suttee, Ashish; Kumar, Santosh; Barnwal, Ravi Pratap; Katare, Om Prakash; Singh, Gurpal

doi:10.1021/acsomega.1c07218

Cited by 5 publications

(2 citation statements)

References 58 publications

(86 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The ability of CDs to potentiate the antibacterial activity of small molecule antibiotics [ 31 ], essential oils [ 32 , 33 ], and other naturally derived antimicrobial compounds [ 34 ] has frequently been demonstrated and is believed to be a direct consequence of increased solubility and, therefore, the bioavailability of hydrophobic active compounds [ 31 , 33 ], which, in this study, are the poorly water-soluble honey solids. Moreover, CD encapsulation can also potentiate the antibacterial effect by minimising the heat- and light-induced degradation and oxidation of the active [ 33 , 35 ] and enabling sustained drug release [ 29 ].…”

Section: Resultsmentioning

confidence: 99%

Preparation and Characterisation of a Cyclodextrin-Complexed Mānuka Honey Microemulsion for Eyelid Application

Rupenthal

Agarwal

et al. 2022

Pharmaceutics

View full text Add to dashboard Cite

Honey has been widely purported as a natural remedy due to its antimicrobial and anti-inflammatory effects. In recent years, several studies have suggested that the considerably high methylglyoxal (MGO) concentration in Mānuka honey (MH) makes it particularly effective to manage bacterial overload, such as that observed in blepharitis. However, the poor solubility, high viscosity, and osmolarity of aqueous honey solutions, especially at the high MGO concentrations studied in the literature, render the formulation of an acceptable dosage form for topical application to the eyelids challenging. Here, the antibacterial properties of raw MH and alpha-cyclodextrin (α-CD)-complexed MH were evaluated at relatively low MGO concentrations, and a liquid crystalline-forming microemulsion containing α-CD-complexed MH was formulated. After determining pH and osmolarity, ocular tolerability was assessed using human primary corneal epithelial cells and chorioallantoic membranes, while the antibacterial efficacy was further evaluated in vitro. The α-CD–MH complex had significantly greater antibacterial activity against Staphylococcus aureus than either constituent alone, which was evident even when formulated as a microemulsion. Moreover, the final formulation had a physiologically acceptable pH and osmolarity for eyelid application and was well-tolerated when diluted 1:10 with artificial tear fluid, as expected to be the case after accidental exposure to the ocular surface in the clinical setting. Thus, a safe and efficient MH dosage form was developed for topical application to the eyelids, which can potentially be used to support optimal eyelid health in the management of blepharitis.

show abstract

Section: Resultsmentioning

confidence: 99%

Preparation and Characterisation of a Cyclodextrin-Complexed Mānuka Honey Microemulsion for Eyelid Application

Rupenthal

Agarwal

et al. 2022

Pharmaceutics

View full text Add to dashboard Cite

show abstract

“…Samples were taken out at predetermined intervals and replaced with fresh media to maintain the sink condition throughout the investigation. Spectrophotometry was used to analyze samples at a maximum wavelength of 232 nm [26].…”

Section: In Vitro Release Of Azithromycin-loaded Preparationsmentioning

confidence: 99%

Development of Tea Tree Oil Based Nanoemulgel Loaded with Azithromycin for Enhancing the Antibacterial Activity

et al. 2023

View full text Add to dashboard Cite

Azithromycin (AZ) is an azalide macrolide antibiotic that is frequently employed for treating bacterial skin infections. It suffers from limited oral bioavailability, which results from incomplete absorption or extensive first-pass metabolism. Therefore, preparing azithromycin formulations for topical administration is highly recommended to avoid first-pass metabolism and to boost the concentration of the drug on the skin. The objective of our investigation was to formulate and evaluate the efficacy of AZ-loaded nanoemulgel as an antimicrobial drug. The physical appearance, spreadability, viscosity, particle size, in vitro drug release, ex vivo permeation investigations, and antimicrobial efficiency of the prepared formulations were evaluated. The prepared formulation loaded with AZ exhibited good physical quality. AZ-loaded nanoemulgel had a greater ex vivo drug permeation across rabbit skin than other formulations (AZ-loaded gel and AZ-loaded emulgel), revealing improved drug permeation and greater transdermal flux in addition to enhanced antibacterial efficacy (p < 0.05). Overall, our findings imply that tea-tree-oil-based nanoemulgel would be a promising delivery system for enhancing the antimicrobial efficiency of azithromycin.

show abstract

Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles

S. Mohamad,

Stephanie,

Sapiun

et al. 2024

ACS Omega

View full text Add to dashboard Cite

Gout is a pathological condition caused by monosodium urate crystal deposition in tissues. Allopurinol, the first-line therapy, inhibits xanthine oxidase but may be ineffective due to reduced conversion to oxypurinol (OXY). Current delivery routes for OXY, including oral and intravenous routes, have drawbacks such as poor solubility and patient discomfort. This study developed a delivery system integrating thermosensitive gel (TRG) containing OXY with polymeric solid microneedles (PSMNs). Molecular docking demonstrated high-affinity binding interactions between OXY and Pluronic (−2.5). The TRG, formulated with Pluronic F127 and F68, was assessed for gelation temperature, pH, spreadability, and bioadhesive strength. PSMN, made from poly(vinyl alcohol) and polyvinylpyrrolidone K-30 with citric acid, was evaluated for mechanical strength and skin penetration. In vitro hemolysis activity, drug release, and ex vivo permeation studies were conducted. Molecular docking results showed stable binding with an affinity of −2.5 between the ligands of OXY and Pluronic. The TRG formulation exhibited promising characteristics for transdermal drug delivery. PSMN demonstrated good mechanical strength and was able to penetrate up to 504 μm. Hemolysis testing showed that PSMN and TSG were safe with a hemolysis ratio of less than 5%. In vitro drug release studies showed a high OXY release of 2.24 ± 0.26 mg with the highest concentration of Pluronic F68, displaying a sustained release profile. Ex vivo permeation studies showed a significant difference (p < 0.05) between OXY permeation without and with PSMN combination. PSMN increased OXY permeation by 79−81% compared to permeation without PSMN. This study successfully developed a TRG formulation combined with PSMN to enhance transdermal delivery of OXY. These results suggest a promising new route for OXY delivery, potentially offering a more efficient and user-friendly treatment for chronic gout. Further in vivo studies are needed to evaluate the efficacy, pharmacokinetics, pharmacodynamics, drug interactions, and toxicity for further clinical applications.

show abstract

Cyclodextrin Derivative Enhances the Ophthalmic Delivery of Poorly Soluble Azithromycin

Cited by 5 publications

References 58 publications

Preparation and Characterisation of a Cyclodextrin-Complexed Mānuka Honey Microemulsion for Eyelid Application

Preparation and Characterisation of a Cyclodextrin-Complexed Mānuka Honey Microemulsion for Eyelid Application

Development of Tea Tree Oil Based Nanoemulgel Loaded with Azithromycin for Enhancing the Antibacterial Activity

Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles

Contact Info

Product

Resources

About