Formulation of sustained release bioadhesive minitablets containing solid dispersion of levofloxacin for once daily ocular use

El-Bary, A. Abd; Ibrahim, Howida Kamal; Haza'a, Balqees Saeed; Sharabi, Ibrahim Al

doi:10.1080/10837450.2019.1602631

Cited by 10 publications

(7 citation statements)

References 59 publications

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“…The process continued until the complete dissolve of the tablet. The swelling index was calculated for each time point using the following equation: 20,22,23 Swelling Index = (Final weight-Initial weight)/(Initial weight)…”

Section: Swelling and Hydration Behaviormentioning

confidence: 99%

Preparation and Characterization of Instantly-soluble Solid Eye Drop for Glaucomatous Patients

Hameed¹,

Al-Shohani²

2023

IJDDT

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For the treatment of glaucoma eye drops are chronically used. However, chronic use of preservatives in eye drops cause irritation problem and aff ects ocular tissues. The aim is to formulate an instant soluble solid eye drop to avoid using preservatives since solid dosage forms do not require preservation. Ocular mini-tablets of dorzolamide hydrochloride (DZ) and timolol maleate (TM) were prepared by direct compression using diff erent polymers and were evaluated for their physical properties. The release DZ and TM was compared to COSOPT eye drops. Formulation F2 mini-tablets (which contain DZ, TM, mannitol and microcrystalline cellulose MCC) were chosen as the optimum formula because they had uniform shape and minimum variation in weight 9.69 ± 0.55 mg. Thickness and diameter were 1.38 ± 1.28 and 3.01 ± 0.03 mm, respectively, within the acceptable limits. Hardness and friability were also within the permissable range which were 4.14 ± 0.22 kg/cm2 for hardness and 0.73% ± 0.05 for friability. The drug content for both DZ and TM were within the acceptable limits and the release had no signifi cant diff erence (p > 0.05) compared to commercial eye drop and the mini-tablets dissolved completely with less than one minute. The FTIR and DSC revealed no interaction between the drugs and excipients used. Sterilization using gamma radiation was performed to test the animal’s mini-tablets. The radiation did not signifi cantly (p > 0.05) alter any properties of F2 and no signs of irritation on the animal eye appeared. In conclusion, instant soluble solid eye drop in the form of mini-tablet was successfully prepared by direct compression method and caused no irritation when tested on animals

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Section: Swelling and Hydration Behaviormentioning

confidence: 99%

Preparation and Characterization of Instantly-soluble Solid Eye Drop for Glaucomatous Patients

Hameed¹,

Al-Shohani²

2023

IJDDT

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“…The drug release profile revealed that Carbopol significantly retarded the drug release of levofloxacin ocular mini-tablets for up to 24 h attributed to its excellent mucoadhesive properties. This is because the gelatinous layer formed on the mini tablets' surface upon wetting, which restrains the drug release from the formulation [19]. Evidently, the incorporation of mucoadhesive polymers increases ocular residence and provides sustained release action upon contact with the mucous membrane.…”

Section: Mucoadhesive Polymeric Approachmentioning

confidence: 99%

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

et al. 2021

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Eyesight is one of the most well-deserved blessings, amid all the five senses in the human body. It captures the raw signals from the outside world to create detailed visual images, granting the ability to witness and gain knowledge about the world. Eyes are exposed directly to the external environment; they are susceptible to the vicissitudes of diseases. The World Health Organization has predicted that the number of individuals affected by eye diseases will rise enormously in the next decades. However, the physical barriers of the eyes and the problems associated with conventional ocular formulations are significant challenges in ophthalmic drug development. This has generated the demand for a sustained ocular drug delivery system, which serves to deliver effective drug concentration at a reduced frequency for consistent therapeutic effect and better patient treatment adherence. Recent advancement in pharmaceutical dosage design has demonstrated that a stimuli-responsive in situ gel system exhibits the favorable characteristics for providing sustained ocular drug delivery and enhanced ocular bioavailability. Stimuli-responsive in situ gels undergo a phase transition (solution–gelation) in response to the ocular environmental temperature, pH, and ions. These stimuli transform the formulation into a gel at the cul de sac to overcome the shortcomings of conventional eye drops, such as rapid nasolacrimal drainage and short contact time with the ocular surface This review highlights the recent successful research outcomes of stimuli-responsive in situ gelling systems in treating in vivo models with glaucoma and various ocular infections. Additionally, it also presents the mechanism, recent development, and safety considerations of stimuli-sensitive in situ gel as the potential sustained ocular delivery system for treating common eye disorders.

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“…Several examples of development and characterization of minitablets with various release types have been described, e.g., (6)(7)(8)(9)(10)(11)(12)(13)(14)(15). However, to the authors' knowledge, reports of comprehensive approach to minitablets' formulation and process optimization in an industrially relevant setting are lacking in the publicly available literature, especially in the topic of ODMTs.…”

Section: Introductionmentioning

confidence: 99%

Implementing the Design of Experiments (DoE) Concept into the Development Phase of Orodispersible Minitablets (ODMTs) Containing Melatonin

et al. 2022

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Development of orodispersible minitablets (ODMTs) requires consideration of aspects related to small dimensions, while ensuring short disintegration time with sufficient mechanical stability. In order to meet these and other critical quality attributes (CQAs), quality by design is encouraged. According to this approach, formulation and compression process factors were systematically studied using design of experiments (Plackett-Burman for screening purposes, full and fractional factorial design for in-depth characterization) to understand their influence on CQAs of orodispersible minitablets containing melatonin. Mathematical models describing the relationships between processing variables and attributes such as resistance to crushing and disintegration time were successfully developed, characterized by high coefficients of determination (R2adj = 0.90–0.97) and prediction errors in the range (+2.4 to −10.8%). In conclusion, based on these models, the design space was created for melatonin ODMTs, ensuring the product’s quality and process robustness. Moreover, the study demonstrated the suitability of texture analysis as an alternative to compendial measurement methods of resistance to crushing and disintegration time.

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Formulation of sustained release bioadhesive minitablets containing solid dispersion of levofloxacin for once daily ocular use

Cited by 10 publications

References 59 publications

Preparation and Characterization of Instantly-soluble Solid Eye Drop for Glaucomatous Patients

Preparation and Characterization of Instantly-soluble Solid Eye Drop for Glaucomatous Patients

Potential of Stimuli-Responsive In Situ Gel System for Sustained Ocular Drug Delivery: Recent Progress and Contemporary Research

Implementing the Design of Experiments (DoE) Concept into the Development Phase of Orodispersible Minitablets (ODMTs) Containing Melatonin

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