Optimization of Thermoreversible<i>In Situ</i>Nasal Gel of Timolol Maleate

Jagdale, Swati; Shewale, Nirupama; Kuchekar, Bhanudas S.

doi:10.1155/2016/6401267

Cited by 30 publications

(21 citation statements)

References 4 publications

(2 reference statements)

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“…The pH values of all the formulations were 6.3–6.5 which were in the nasal physiological pH range 4.5–6.5 ( Table 7 ) [ 64 ].The drug and agents didn’t effects the pH of the formulations. The drug contents of all optimized formulations were checked and found in the range of 97–101% ( Table 8 ).…”

Section: Discussionmentioning

confidence: 99%

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%

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

et al. 2017

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“…This procedure was performed in triplicate. 13,14 Gelling Temperature and Gelation time: Gelation temperature was measured by visual inspection method. Five ml aliquot of gel was taken in a test tube and placed on a thermostatic water bath (Bio-technics, India).…”

Section: Evaluation Parameters Of Nasal Formulationmentioning

confidence: 99%

Xyloglucan Based Nasal in situ Gel Formulation of Mirtazapine for Treatment of Depression

Naresh¹,

Dilip²,

Sunil³

2020

IJPER

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Objectives: The objective of the present work was formulation of thermosensitive mucoadhesive in situ nasal gel of Mirtazapine for depression. The nasal route would overcome the first-pass effect and would enhance its efficacy. Methods: The thermally triggered in situ nasal gel was prepared by cold method using Poloxamer 407 and Xyloglucan. Formulation batches of in situ gel were prepared by using 3 2 full factorial design. The in situ gel was evaluated for gelling temperature, % drug content, ex vivo permeation study and pharmacodynamic study. Results: The differential scanning calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy of drug and physical mixture showed compatibility. Drug content and gelling temperature of optimized batch was found to be 85.22-95.92 % and 30-35°C respectively. Ex vivo permeation of optimized formulation F4 was found to be 91.89%. Pharmacodynamic study was performed using despair forced swim test and locomotor activity on mice and it was found that in situ nasal gel of Mirtazapine was more effective than that of the marketed formulation. Stability studies revealed that the optimized formulation was stable. Conclusion: The prepared in situ nasal gel of Mirtazapine enhanced the residence time in the nostrils and enhanced the therapeutic efficacy by avoidance of first-pass metabolism.

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“…The intra nasal route has been used for the delivery of several drugs 12 . However, there is only one report on the possibility of antihypertensive drug (timolol) administration via this route 13 .…”

Section: Mucosal Administration Routementioning

confidence: 99%

Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice

Biały¹,

Wojcik²,

Młynarczuk-Biały³

2018

BIOMED PAP

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Patients who are unable to receive oral medication (p.o.) are a major problem in outpatient settings, especially in home health care systems. Mucosal administration of drugs offers an alternative to the oral route, especially when the parenteral mode cannot be used. There are three main pathways of mucosal administration: sublingual/buccal, intranasal and rectal. We discuss the possibility of mucosal delivery of antihypertensive drugs. Perindopril arginine and Amlodipine besylate are registered in the EU as orodispersible tablets for oromucosal delivery, however, they are not available in all countries. For this reason, we describe other drugs suitable for mucosal delivery: Captopril and Nitrendipine in the sublingual system and Metoprolol tartrate, Propranolol and Furosemide by the transrectal route. Based on the published data and common clinical practice we discuss the use of mucosal delivery systems of all these antihypertensive drugs with special attention to their pharmacokinetics. We illustrate this mini-review with a case report of the prolonged-term use of mucosal delivery of sublingual Captopril and Nitrendipine combined with rectal Metoprolol tartrate and Furosemide in a patient with severe hypertension unable to receive medication p.o. This is also a report on the first human use of Furosemide-containing suppositories as well as prolonged-term transmucosal administration of these four drugs, describing a practical approach leading to successful control of severe hypertension with four antihypertensive drugs delivered via the mucosal route. The treatment was effective and without side effects; however, the long-term safety and efficacy of such therapy must be confirmed by randomized clinical trials.

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Optimization of ThermoreversibleIn SituNasal Gel of Timolol Maleate

Cited by 30 publications

References 4 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

Xyloglucan Based Nasal in situ Gel Formulation of Mirtazapine for Treatment of Depression

Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice

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