Design of Topical Moxifloxacin Mucoadhesive Nanoemulsion for the Management of Ocular Bacterial Infections

Youssef, Ahmed Adel Ali; Thakkar, Ruchi; Senapati, Samir; Joshi, Poorva H.; Dudhipala, Narendar; Majumdar, Soumyajit

doi:10.3390/pharmaceutics14061246

Cited by 11 publications

(7 citation statements)

References 56 publications

(83 reference statements)

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“…Each of the three release models (Korsmeyer–Peppas, Higuchi, and first-order), and regression analysis were carried out for each formulation profile to assess the best fit based on its coefficient of determination (R 2 ) [ 23 ]. The release model with the highest R 2 was chosen as the best model to describe release kinetics ( Table 5 ).…”

Section: Resultsmentioning

confidence: 99%

“…The mobile phase was pumped isocratically at 1.2 mL/min through a Waters Symmetry ® (150 × 4.6 mm, 5 μm) C 18 column set at 25 °C, with a detection wavelength (λ max ) set at 294 nm. The samples were analyzed using a Waters chromatography data system coupled with Empower software [ 23 ]. The analytical method was linear over a GTX concentration range of 1–100 μg/mL.…”

Section: Methodsmentioning

confidence: 99%

“…An accurately weighed amount (10 mg) of GTX was added to each liquid or solid lipid (200 mg) in separate glass vials (3 mL). This mixture was stirred at 2000 rpm under ambient temperature (80 ± 2 °C) for 10 min [ 23 ]. After 10 min, stirring was discontinued and the mixtures were removed from the heat.…”

Section: Methodsmentioning

confidence: 99%

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Gatifloxacin Loaded Nano Lipid Carriers for the Management of Bacterial Conjunctivitis

Joshi,

Youssef,

Ghonge

et al. 2023

Antibiotics

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Bacterial conjunctivitis (BC) entails inflammation of the ocular mucous membrane. Early effective treatment of BC can prevent the spread of the infection to the intraocular tissues, which could lead to bacterial endophthalmitis or serious visual disability. In 2003, gatifloxacin (GTX) eyedrops were introduced as a new broad-spectrum fluoroquinolone to treat BC. Subsequently, GTX use was extended to other ocular bacterial infections. However, due to precorneal loss and poor ocular bioavailability, frequent administration of the commercial eyedrops is necessary, leading to poor patient compliance. Thus, the goal of the current investigation was to formulate GTX in a lipid-based drug delivery system to overcome the challenges with the existing marketed eyedrops and, thus, improve the management of bacterial conjunctivitis. GTX-NLCs and SLNs were formulated with a hot homogenization–probe sonication method. The lead GTX-NLC formulation was characterized and assessed for in vitro drug release, antimicrobial efficacy (against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa), and ex vivo permeation. The lead formulation exhibited desired physicochemical characteristics, an extended release of GTX over a 12 h period, and was stable over three months at the three storage conditions (refrigerated, room temperature, and accelerated). The transcorneal flux and permeability of GTX from the GTX-NLC formulation were 5.5- and 6.0-fold higher in comparison to the commercial eyedrops and exhibited a similar in vitro antibacterial activity. Therefore, GTX-NLCs could serve as an alternative drug delivery platform to improve treatment outcomes in BC.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Gatifloxacin Loaded Nano Lipid Carriers for the Management of Bacterial Conjunctivitis

Joshi,

Youssef,

Ghonge

et al. 2023

Antibiotics

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“…Hot homogenization coupled with the ultrasonication method was employed in the preparation of IR-SLN and IR-HPβCD-SLN dispersion 20 . The oily phase of IR-SLNs was prepared by dissolving IR (0.1% w/v), solid lipid (Dynasan 112, 2% w/v), and soylecithin (2% w/v) in chloroform and methanol mixture (5 ml, 1:1).…”

Section: Methodsmentioning

confidence: 99%

Development and In vivo Pharmacokinetic and Pharmacodynamic Evaluation of an Oral Innovative Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan Formulation for Enhanced Bioavailability

Dudhipala¹,

Ettireddy²,

Youssef³

et al. 2023

Nanotheranostics

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Background: Irbesartan (IR) is used in the treatment of hypertension, heart failure, and nephropathy in Type II diabetes. IR bioavailability is limited by poor solubility and presystemic metabolism. In our previous investigations, cyclodextrin (HPβCD) complexed solid lipid nanoparticles (SLNs) of IR were prepared, optimized, and characterized. The current study aimed to confirm the reproducibility of the previous methodology and to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) performance of the selected lead formulations in an experimental animal model. Methods: SLNs were prepared by hot homogenization followed by probe sonication with IR/HPβCD inclusion complex loaded into a solid lipid (Dynasan 112). SLNs were evaluated for physical characteristics, drug content, entrapment efficiency, in vitro release profile, and surface morphology. The pharmacokinetic and pharmacodynamic behavior of the SLNs were evaluated in Wistar rats. Results: Photon correlation spectroscopy, drug content, entrapment efficiency, and dissolution studies results were reproducible and consistent with our earlier investigation. PK studies showed 2.1-, 6.6-, and 9.9-fold improvement in the relative oral bioavailability of the drug from IR-HPβCD, IR-SLN, and IR-HPβCD-SLN formulations, respectively compared to IR suspension. However, IR-HPβCD-SLNs showed 1.5-and 4.7-fold improvement in the relative oral bioavailability of the drug compared to IR-SLN and IR-HPβCD formulations, respectively. PD studies in hypertensive Wistar rats showed a good control over systolic blood pressure for 48 h for SLN formulations compared to 2 h for IR suspension. However, the IR-HPβCD inclusion complex exhibited immediate antihypertensive activity (0.5 h) with a period of systolic blood pressure control similar to IR suspension. Conclusions: The current approach exhibited improved oral bioavailability along with improved and prolonged pharmacodynamic effect.

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“…The entrapment of QTF molecules within the formed nanoemulsion oil globules and slow drug diffusion from the oil phase to the aqueous phase could contribute to the extended-release behavior from the SNEDDS formulation. The release of hydrophobic drugs from this O/W NE type involves two consecutive steps, starting with the partitioning (diffusion) of the loaded hydrophobic drug from the oil phase into surfactant and then into the aqueous dissolution medium, thus extending the drug release from these drug delivery systems [41]. In order to understand the drug release mechanism from the optimized S-SNEDDS formulation, the release data were fitted to four conventional release models using the DDSolver software, as shown in Table 10.…”

Section: Dissolution Studiesmentioning

confidence: 99%

Formulation Development of Solid Self-Nanoemulsifying Drug Delivery Systems of Quetiapine Fumarate via Hot-Melt Extrusion Technology: Optimization Using Central Composite Design

Uttreja,

Youssef,

Karnik

et al. 2024

Pharmaceutics

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Quetiapine fumarate (QTF) was approved for the treatment of schizophrenia and acute manic episodes. QTF can also be used as an adjunctive treatment for major depressive disorders. QTF oral bioavailability is limited due to its poor aqueous solubility and pre-systemic metabolism. The objective of the current investigation was the formulation development and manufacturing of solid self-nanoemulsifying drug delivery system (S-SNEDDS) formulation through a single-step continuous hot-melt extrusion (HME) process to address these drawbacks. In this study, Capmul® MCM, Gelucire® 48/16, and propylene glycol were selected as oil, surfactant, and co-surfactant, respectively, for the preparation of S-SNEDDS. Soluplus® and Klucel™ EF (1:1) were selected as the solid carrier. Response surface methodology in the form of central composite design (CCD) was utilized in the current experimental design to develop the S-SNEDDS formulations via a continuous HME technology. The developed formulations were evaluated for self-emulsifying properties, particle size distribution, thermal behavior, crystallinity, morphology, physicochemical incompatibility, accelerated stability, and in vitro drug release studies. The globule size and emulsification time of the optimized SNEDDS formulation was 92.27 ± 3.4 nm and 3.4 ± 3.38 min. The differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies revealed the amorphous nature of the drug within the formulation. There were no drug-excipient incompatibilities observed following the Fourier transform infrared (FTIR) spectroscopy. The optimized formulation showed an extended-release profile for 24 h. The optimized formulation was stable for three months (last time-point tested) at 40 °C/75% RH. Therefore, the developed S-SNEDDS formulation could be an effective oral delivery platform for QTF and could lead to better therapeutic outcomes.

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Design of Topical Moxifloxacin Mucoadhesive Nanoemulsion for the Management of Ocular Bacterial Infections

Cited by 11 publications

References 56 publications

Gatifloxacin Loaded Nano Lipid Carriers for the Management of Bacterial Conjunctivitis

Gatifloxacin Loaded Nano Lipid Carriers for the Management of Bacterial Conjunctivitis

Development and In vivo Pharmacokinetic and Pharmacodynamic Evaluation of an Oral Innovative Cyclodextrin Complexed Lipid Nanoparticles of Irbesartan Formulation for Enhanced Bioavailability

Formulation Development of Solid Self-Nanoemulsifying Drug Delivery Systems of Quetiapine Fumarate via Hot-Melt Extrusion Technology: Optimization Using Central Composite Design

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