Formulation and evaluation of thermoreversible, mucoadhesive in situ intranasal gel of rizatriptan benzoate

Kempwade, Amolkumar Ashok; Taranalli, Ashok D

doi:10.1007/s10971-014-3422-5

Cited by 29 publications

(11 citation statements)

References 10 publications

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“…Nasal drug delivery has received a significant attention as a convenient and reliable route for local administration of drugs [ 43 , 44 ]. The nasal cavity offered a distinctive advantage for potential direct drug delivery to the brain along the olfactory nerves [ 34 , 45 , 46 ]. The rapid mucociliary clearance was important rate-limiting factor for nasal drug absorption [ 15 , 47 ].…”

Section: Discussionmentioning

confidence: 99%

“…Determination of gelation temperature is a major step in the preparation of the thermoreversible gel [ 51 , 52 ]. The thermoreversible hydrogel for nasal drug delivery should be gelled in 25–34°C [ 23 , 53 ].…”

Section: Discussionmentioning

confidence: 99%

“…The gel strength of formulation was determined as reported previously [ 32 – 34 ]. A sample of 50 g of hydrogel was put into a 100 ml graduated cylinder and gelled in a thermostatically controlled water bath at 37±0.5°C.…”

Section: Methodsmentioning

confidence: 99%

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A mucoadhesive, thermoreversible in situ nasal gel of geniposide for neurodegenerative diseases

et al. 2017

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Neurodegenerative diseases are becoming prevalent as the population ages. Geniposide could inhibit oxidative stress, reduce apoptosis, protect neuron, and has been used for therapy of the neurodegenerative diseases. The bioavailability of geniposide by nasal route is greater than that by oral administration. However, mucociliary clearance is a rate-limiting factor for nasal route administration. The objective of this study was to develop and evaluate a mucoadhesive, thermoreversible in situ nasal gel of geniposide. The poloxamers (P407, P188) and the hydroxypropyl methylcellulose were used as thermoreversible and mucoadhesive polymers, respectively. Borneol was used as a permeation enhancer. The hydrogel was prepared with the cold method and optimized by the response surface methodology-central composite design. Gelation temperature, pH, clarity, gel strength, mucoadhesive strength, in vitro and ex vivo release kinetics of formulations were evaluated. The optimized amounts of poloxamer407 (P407), poloxamer188 (P188) and hydroxypropyl methylcellulose were determined to be 19.4–20.5%, 1.1–4.0% and 0.3–0.6% respectively. The second-order polynomial equation in terms of actual factors indicated a satisfactory correlation between the independent variables and the response (R2 = 0.9760). An ANOVA of the empirical second-order polynomial model indicated the model was significant (P<0.01). P407, P188, P407×P188, P4072 and P1882 were significant model terms. The effects of P407 on gelation temperature were greater than those of other independent variables. The pH values of all the formulations were found to be within 6.3–6.5 which was in the nasal physiological pH range 4.5–6.5. The drug content, gel strength, mucoadhesive strength of the optimized formulations were 97–101%, 25–50 sec and 4000–6000 dyn/cm2 respectively. The in vitro release kinetics of cumulative release of geniposide was fitted to the zero-order model. The ex vivo cumulative release kinetics of geniposide was fitted to the Weibull model. This study concludes that the release of geniposide is controlled by gel corrosion, and that the permeation of geniposide is time-dependent. The more residence time, mucoadhesive, thermoreversible in situ nasal gel of geniposide for neurodegenerative diseases is of compliance and potential application.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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A mucoadhesive, thermoreversible in situ nasal gel of geniposide for neurodegenerative diseases

et al. 2017

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“…In the last decade, several authors have investigated the use of thermo-sensitive formulations for the nasal administration of anti-migraine drugs, such as sumatriptan [ 60 ], rizatriptan benzoate [ 61 ] and zolmitriptan [ 62 ]. Shelke et al [ 63 ] developed an in situ gelling bioadhesive formulation consisting of P407 and C934 for naratriptan hydrochloride (NH) delivery to the brain via the olfactory lobe pathway.…”

Section: Nasal Routementioning

confidence: 99%

Recent Advances in the Development of In Situ Gelling Drug Delivery Systems for Non-Parenteral Administration Routes

et al. 2020

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In situ gelling drug delivery systems have gained enormous attention over the last decade. They are in a sol-state before administration, and they are capable of forming gels in response to different endogenous stimuli, such as temperature increase, pH change and the presence of ions. Such systems can be administered through different routes, to achieve local or systemic drug delivery and can also be successfully used as vehicles for drug-loaded nano- and microparticles. Natural, synthetic and/or semi-synthetic polymers with in situ gelling behavior can be used alone, or in combination, for the preparation of such systems; the association with mucoadhesive polymers is highly desirable in order to further prolong the residence time at the site of action/absorption. In situ gelling systems include also solid polymeric formulations, generally obtained by freeze-drying, which, after contact with biological fluids, undergo a fast hydration with the formation of a gel able to release the drug loaded in a controlled manner. This review provides an overview of the in situ gelling drug delivery systems developed in the last 10 years for non-parenteral administration routes, such as ocular, nasal, buccal, gastrointestinal, vaginal and intravesical ones, with a special focus on formulation composition, polymer gelation mechanism and in vitro release studies.

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“…Several formulation approaches have been investigated to overcome these hurdles and obtain prolonged residence time and sustained nasal drug release, and, among these, in-situ gel forming systems appear as particularly attractive [ 16 , 17 ]. Among the different environmentally responsive systems investigated, thermosensitive hydrogels with lower critical gelation temperature (LCGT) close to the physiological temperature range are the most used [ 18 , 19 , 20 , 21 ]. They have the advantage of being fluid at ambient temperature, thus being easily administrable with high dose accuracy by nasal drops.…”

Section: Introductionmentioning

confidence: 99%

Development of a Cyclodextrin-Based Mucoadhesive-Thermosensitive In Situ Gel for Clonazepam Intranasal Delivery

et al. 2021

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A thermosensitive, mucoadhesive in-situ gel for clonazepam (CLZ) intranasal delivery was developed, which aimed to achieve prolonged in-situ residence and controlled drug release, overcoming problems associated with its oral or parenteral administration. Poloxamer was selected as a thermosensitive polymer and chitosan glutamate and sodium hyaluronate as mucoadhesive and permeation enhancer. Moreover, randomly methylated β-Cyclodextrin (RAMEB) was used to improve the low drug solubility. A screening DoE was applied for a systematic examination of the effect of varying the formulation components proportions on gelation temperature, gelation time and pH. Drug-loaded gels at different clonazepam-RAMEB concentrations were then prepared and characterized for gelation temperature, gelation time, gel strength, mucoadhesive strength, mucoadhesion time, and drug release properties. All formulations showed suitable gelation temperature (29–30.5 °C) and time (50–65 s), but the one with the highest drug-RAMEB concentration showed the best mucoadhesive strength, longest mucoadhesion time (6 h), and greatest release rate. Therefore, it was selected for cytotoxicity and permeation studies through Caco-2 cells, compared with an analogous formulation without RAMEB and a drug solution. Both gels were significantly more effective than the solution. However, RAMEB was essential not only to promote drug release, but also to reduce drug cytotoxicity and further improve its permeability.

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Formulation and evaluation of thermoreversible, mucoadhesive in situ intranasal gel of rizatriptan benzoate

Cited by 29 publications

References 10 publications

A mucoadhesive, thermoreversible in situ nasal gel of geniposide for neurodegenerative diseases

A mucoadhesive, thermoreversible in situ nasal gel of geniposide for neurodegenerative diseases

Recent Advances in the Development of In Situ Gelling Drug Delivery Systems for Non-Parenteral Administration Routes

Development of a Cyclodextrin-Based Mucoadhesive-Thermosensitive In Situ Gel for Clonazepam Intranasal Delivery

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