Poloxamer/Cyclodextrin/Chitosan-Based Thermoreversible Gel for Intranasal Delivery of Fexofenadine Hydrochloride

Cho, Hyun‐Jong; Balakrishnan, Pachamuthu; Park, Eun-Kyoung; Song, Kihyung; Hong, Sung Kyung; Jang, T.; Kim, Kyu-Sung; Chung, Suk‐Jae; Shim, Chang‐Koo; Kim, Dae‐Duk

doi:10.1002/jps.22314

Cited by 68 publications

(57 citation statements)

References 38 publications

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“…[1][2][3][4] The viscosity of this type of system can be modulated by the amount of water it contains, 5 by temperature, and by pH changes 6 and can undergo a transition to gel on contact with the bodily fluid at a mucosal site. 1 The administration of the drug delivery system (DDS) into confined spaces, for example, within the vaginal 7,8 and nasal 1,9 cavities, periodontal pocket, 10,11 or conjunctival sac, 2 is a complex task and remains as a challenge for formulation scientists.…”

Section: Introductionmentioning

confidence: 99%

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Nunes

Teixeira

Kaminski

et al. 2016

Journal of Pharmaceutical Sciences

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This article reports the development of a precursor liquid crystalline system based on a mixture of monoglycerides (MO) and Cremophor(®) (CREM) that exhibits in situ gelation to a liquid crystalline phase. The effects of different MO/CREM ratios and the water content (WC) on several performance characteristics were investigated with a full factorial design. The formulations were characterized by polarized light microscopy, small-angle X-ray scattering, and water uptake assays. Rheological, syringeability, and mucoadhesion evaluation were also performed. The polarized light microscopy and small-angle X-ray scattering results for average and high MO/CREM ratios (2.1 and 4.0, respectively) indicated the coexistence of phases in transition to the liquid crystalline phase, independently of the WC. These systems became more viscous after taking up water, showing peaks characteristic of a cubic phase. Systems that had average and high MO/CREM ratios also exhibited shear-thinning behavior and high elasticity. Most systems showed suitable mucoadhesion for buccal purposes. Response surface methodology results demonstrated that the relative contribution of MO was the principal factor that affected the performance of the system. Accordingly, these precursor systems with average to high MO/CREM ratios and an average WC (10% w/w) demonstrated physicochemical and mucoadhesive properties that could enable them to be used as an in situ-gelling controlled drug delivery platform.

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Section: Introductionmentioning

confidence: 99%

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Nunes

Teixeira

Kaminski

et al. 2016

Journal of Pharmaceutical Sciences

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“…The initial screening and optimisation resulting in 32 formulations, of which 3 demonstrated optimal gelation at the nasal cavity temperature of 34 °C ± 1°C 54 . These formulations were identified as FCMC (1 % w/v CMC), FPEG (1 % w/v PEG4000) and FCS (0.1 % w/v chitosan) and which all contained 17 % w/v P172 and 1% w/v amantadine (in addition to excipients).…”

Section: Sol-gel Transition (Tsol-gel)mentioning

confidence: 99%

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

Lungare

Bowen

Badhan

2016

Journal of Pharmaceutical Sciences

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The aim of this study was to develop and characterise an intranasal delivery system for amantadine (AMT). Optimal formulations (F) consisted of a thermosensitive polymer Pluronic ® 127 (P127) and either carboxy methyl cellulose (CMC) or chitosan (CS) which demonstrated gel-transition at nasal cavity temperatures (34 °C ± 1 °C). Rheologically, the loss tangent (Tan δ) confirmed a three-stage gelation phenomena at 34 °C ± 1 °C and nonNewtonian behaviour. Storage of FCMC and FCS at 4 °C for 8 weeks resulted in repeatable release profiles at 34 °C when sampled, with a Fickian mechanism earlier on but moving towards anomalous transport by week 8. Polymers (P127, CMC and CS) demonstrated no significant cellular toxicity to human nasal epithelial cells up to 4 mg/mL and up to 1 mM for AMT (IC50: 4.5 mM ± 0.05 mM). FCMC and FCS demonstrated slower release across an in-vitro human nasal airway model (43-44 % vs 79 % ± 4.58 % for AMT). Using a human nasal cast model, deposition into the olfactory regions (potential nose-to-brain) was demonstrated upon nozzle insertion (5 mm) whereas tilting of the head forward (15°) resulted in greater deposition in the bulk of the nasal cavity. KEYWORDSParkinson's disease; rheology; nasal; RPMI 2650; nose to brain; thermoresponsive; 3 INTRODUCTION Parkinson's disease (PD) is an ageing associated progressive neurological disorder and affects 1.5 % of the population over 65-years of age 1 , with age-adjusted prevalence rates thought to be around 150 per 100,000 with a suggested mean onset in the 70's 1 . Ageing is the largest single risk factor for the development of PD and the pathogenesis of PD is composed of a range of events leading towards neuronal apoptosis, primarily of degradation of dopamine neurones in the sustantia nigra. The mainstay of clinical drug therapy focuses on increases the levels of dopamine (DA) in the brain, with oral dosing of levodopa being the most commonly used to pharmacological intervention treatment to reverse the symptoms of PD. It is also common to use adjunct therapies in conjunction with levodopa, such as the weak NMDA-type receptor antagonist amantadine, which can aid in blocking dopamine reuptake.

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“…Their studies showed an improved bioavailability of fexofenadine hydrochloride in animal model (i.e. rabbit) owing to the fact that chitosan and hydroxypropyl-β-cyclodextrin are permeation enhancers [151].…”

Section: Polysaccharide-based Nasal Delivery Systemsmentioning

confidence: 99%

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

Boateng

Okeke²,

Khan³

2015

CPD

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There has been increased interest in novel drug delivery systems to be administered via mucosal routes as an alternative to the currently used traditional routes such as parenteral (injections) and oral routes of administration. This is due to the several advantages they offer including avoiding first pass metabolism in the liver for oral administration and local activity which avoids the need for high systemic doses. To achieve the foregoing objectives, bioadhesive vehicles are required that ensure prolonged residence time to achieve systemic bioavailability via substantial drug absorption or significant drug concentration for local action.The drug delivery system is also required to be non-deleterious to the site of application and be well tolerated by vulnerable groups such as paediatric and geriatric patients. These essential characteristics are mainly satisfied by naturally occurring polymers, including polysaccharide based polymers which have the advantage of biocompatibility, biodegradability and therefore safety. This review discusses various bioadhesive polymers of polysaccharide origin formulated into a variety of dosage forms for drug delivery via the body's mucosal (moist) surfaces including ocular, oral (buccal and sublingual), nasal, gastrointestinal and vaginal mucosa, as well as moist wound sites. The anatomy and / or physiology of each site, coupled with the unique challenges each poses, the strategies employed for ensuring therapeutic efficacy, as well as the current state of the art will also be covered.

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Poloxamer/Cyclodextrin/Chitosan-Based Thermoreversible Gel for Intranasal Delivery of Fexofenadine Hydrochloride

Cited by 68 publications

References 38 publications

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

The Monoglyceride Content Affects the Self-Assembly Behavior, Rheological Properties, Syringeability, and Mucoadhesion of In Situ–Gelling Liquid Crystalline Phase

Development and Evaluation of a Novel Intranasal Spray for the Delivery of Amantadine

Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review

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