Quality by design approach for development and optimization of Quetiapine Fumarate effervescent floating matrix tablets for improved oral bioavailability

Dudhipala, Narendar; Arjun, Nadarajan; Someshwar, Komuravelly; Rao, Yi

doi:10.1007/s40005-016-0232-5

Cited by 31 publications

(11 citation statements)

References 16 publications

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“…In order to find the possible release pattern from optimized CIP-NLC, CIP-NLC-IG2, and CIP-C formulations, the release data were analyzed to check the goodness of fit for zero-order release, first-order release, Higuchi [ 63 , 64 ] and Korsmeyer–Peppas model [ 40 , 65 ]. The model that showed the highest R 2 value was considered as the best model to describe release kinetics.…”

Section: Resultsmentioning

confidence: 99%

Ciprofloxacin Loaded Nanostructured Lipid Carriers Incorporated into In-Situ Gels to Improve Management of Bacterial Endophthalmitis

2020

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Bacterial endophthalmitis (BE) is a potentially sight-threatening inflammatory reaction of the intraocular fluids or tissues caused by bacteria. Ciprofloxacin (CIP) eye drops are prescribed as first-line therapy in BE. However, frequent administration is necessary due to precorneal loss and poor ocular bioavailability. The objective of the current research was to prepare CIP containing nanostructured lipid carriers (CIP-NLCs) loaded an in situ gel system (CIP-NLC-IG) for topical ocular administration for enhanced and sustained antibacterial activity in BE treatment. CIP-NLCs were prepared by the hot homogenization method and optimized based on physicochemical characteristics and physical stability. The optimized CIP-NLC formulation was converted into CIP-NLC-IG with the addition of gellan gum as a gelling agent. Furthermore, optimized CIP-NLC and CIP-NLC-IG were evaluated for in vitro release and ex vivo transcorneal permeation studies, using commercial CIP ophthalmic solution (CIP-C) as the control. The optimized CIP-NLC formulation showed particle size, polydispersity index, zeta potential, assay and entrapment efficiency of 193.1 ± 5.1 nm, 0.43 ± 0.01, −32.5 ± 1.5 mV, 99.5 ± 5.5 and 96.3 ± 2.5%, respectively. CIP-NLC-IG with 0.2% w/v gellan gum showed optimal viscoelastic characteristics. The in vitro release studies demonstrated sustained release of CIP from CIP-NLC and CIP-NLC-IG formulations over a 24 h period. Transcorneal flux and permeability increased 4 and 3.5-fold, and 2.2 and 1.9-fold from CIP-NLC and CIP-NLC-IG formulations, respectively, when compared to CIP-C. The results demonstrate that CIP-NLC-IG could be considered as an alternate delivery system to prolong the residence time on the ocular surface after topical administration. Thus, the current CIP ophthalmic formulations may exhibit improved ocular bioavailability and prolonged antibacterial activity, which may improve therapeutic outcomes in the treatment of BE.

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Section: Resultsmentioning

confidence: 99%

Ciprofloxacin Loaded Nanostructured Lipid Carriers Incorporated into In-Situ Gels to Improve Management of Bacterial Endophthalmitis

2020

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“…Undesired dissolution may result in unexpected bioavailability [ 36 ]. Inappropriate tablet hardness can affect safety and efficacy [ 37 ]. Friability of less than 1.0% w / w can reduce the impact on patient safety and efficacy [ 36 ].…”

Section: Resultsmentioning

confidence: 99%

Control Strategy for Process Development of High-Shear Wet Granulation and Roller Compaction to Prepare a Combination Drug Using Integrated Quality by Design

2021

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In this study, we developed a control strategy for a drug product prepared by high-shear wet granulation and roller compaction using integrated quality by design (QbD). During the first and second stages, we optimized the process parameters through the design of experiments and identified the intermediate quality attributes (IQAs) and critical quality attributes (CQAs) relationship, respectively. In the first stage, we conducted an initial risk assessment by selecting critical process parameters with high impact on IQAs and CQAs and confirmed the correlation between control and response factors. Additionally, we performed Monte Carlo simulations by optimizing the process parameters to deriving and building a robust design space. In the second stage, we identified the IQAs and CQAs relationship for the control strategy, using multivariate analysis (MVA). Based on MVA, in the metformin layer, dissolution at 1 h was significantly correlated with intrinsic dissolution rate and granule size, and dissolution at 3 h was significantly correlated with bulk density and granule size. In dapagliflozin layer, dissolution at 10 min and 15 min was significantly correlated with granule size. Our results suggest that the desired drug quality may result through IQAs monitoring during the process and that the integrated QbD approach utilizing MVA can be used to develop a control strategy for producing high-quality drug products.

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“…Data for regression analysis were processed using the statistical function of Microsoft ® (MS) office excel (Office365, 2019, USA). To study the mechanism of drug release from NE, Zero-order, First-order, Higuchi, and Korsmeyer–Peppas equations [ 67 , 68 ] were chosen as mathematical models to characterize the in vitro release profile. These models are commonly used to describe the drug release pattern from drug delivery systems when the drug release mechanism is not clear or when there is more than one type of release phenomenon involved.…”

Section: Methodsmentioning

confidence: 99%

Design of Topical Ocular Ciprofloxacin Nanoemulsion for the Management of Bacterial Keratitis

et al. 2021

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Bacterial keratitis (BK) is a critical ocular infection that can lead to serious visual disability. Ciprofloxacin (CIP), moxifloxacin (MOX), and levofloxacin (LFX) have been accepted as monotherapies by the US Food and Drug Administration for BK treatment. CIP is available commercially at 0.3% w/v concentration as an ophthalmic solution and as an ointment for ocular delivery. Because of solubility issues at physiological pH, CIP precipitation can occur at the corneal surface post instillation of the solution dosage form. Consequently, the ocular bioavailability of CIP is reduced. The ointment dosage form is associated with side effects such as blurred vision, itching, redness, eye discomfort, and eye dryness. This study aimed to design a CIP loaded nanoemulsion (NE; CIP-NE) to facilitate drug penetration into the corneal layers for improved therapeutic outcomes as well as to overcome the drawbacks of the current commercial ophthalmic formulations. CIP-NE formulations were prepared by hot homogenization and ultrasonication, using oleic acid (CIP-O-NE) and Labrafac® Lipophile WL 1349 (CIP-L-NE) as the oily phase, and Tween® 80 and Poloxamer 188 as surfactants. Optimized CIP-NE was further evaluated with respect to in vitro release, ex vivo transcorneal permeation, and moist heat sterilization process, using commercial CIP ophthalmic solution as a control. Optimized CIP-O-NE formulation showed a globule size, polydispersity index, and zeta potential of 121.6 ± 1.5 nm, 0.13 ± 0.01, and −35.1 ± 2.1 mV, respectively, with 100.1 ± 2.0 % drug content and was spherical in shape. In vitro release and ex vivo transcorneal permeation studies exhibited sustained release and a 2.1-fold permeation enhancement, respectively, compared with commercial CIP ophthalmic solution. Autoclaved CIP-O-NE formulation was found to be stable for one month (last time-point tested) at refrigerated and room temperature. Therefore, CIP-NE formulation could serve as an effective delivery system for CIP and could improve treatment outcomes in BK.

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Quality by design approach for development and optimization of Quetiapine Fumarate effervescent floating matrix tablets for improved oral bioavailability

Cited by 31 publications

References 16 publications

Ciprofloxacin Loaded Nanostructured Lipid Carriers Incorporated into In-Situ Gels to Improve Management of Bacterial Endophthalmitis

Ciprofloxacin Loaded Nanostructured Lipid Carriers Incorporated into In-Situ Gels to Improve Management of Bacterial Endophthalmitis

Control Strategy for Process Development of High-Shear Wet Granulation and Roller Compaction to Prepare a Combination Drug Using Integrated Quality by Design

Design of Topical Ocular Ciprofloxacin Nanoemulsion for the Management of Bacterial Keratitis

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