Ex vivo permeation characteristics of venlafaxine through sheep nasal mucosa

Pund, Swati; Rasve, Ganesh; Borade, Ganesh

doi:10.1016/j.ejps.2012.10.029

Cited by 98 publications

(51 citation statements)

References 29 publications

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“…When n is equal to 0.5, the fraction of the drug released is proportional to the square root of time (Higuchi kinetics) and the drug release is solely controlled by diffusion (Fickian diffusion kinetics). A value n=1 indicates drug release is controlled by swelling, a case-II transport (zero-order kinetics), while the value 0.5<n<1 indicates anomalous transport and superposition of both phenomena (non-Fickian kinetic) 48. For the majority of the prepared formulations, the values of n were found to be approximately 1, indicating case-II transport where the drug release involves polymer relaxation and chain disentanglement 49.…”

Section: Resultsmentioning

confidence: 96%

“…The Korsmeyer–Peppas model was used to explain the mechanism of drug release from the prepared tablet formulations 48. The empirical Korsmeyer–Peppas power law equation is given as M t / M ∞ = K t n , where M t is the amount of drug released at time t, M ∞ is the amount released at time ∞, M t / M ∞ is the fraction of drug released at time t, K is a constant characteristic of the drug–polymer system and n is the diffusional exponent, a measure of the primary mechanism of drug release.…”

Section: Resultsmentioning

confidence: 99%

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Transbuccal delivery of betahistine dihydrochloride from mucoadhesive tablets with a unidirectional drug flow: in vitro, ex vivo and in vivo evaluation

El-Nabarawi¹,

Ali²,

Aboud³

et al. 2016

DDDT

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ObjectiveBetahistine dihydrochloride (BH.2HCl), an anti-vertigo histamine analog used in the treatment of Ménière’s disease, undergoes extensive first-pass metabolism and suffers from short biological half-life. The aim of the present work was to develop and estimate controlled release mucoadhesive buccal tablets of BH.2HCl with a unidirectional drug flow to overcome this encumbrance.MethodsA direct compression method was adopted for preparation of the tablets using mucoadhesive polymers like guar gum, hydroxypropyl methyl cellulose K4M, sodium carboxymethyl cellulose and their combinations. The tablets were coated from all surfaces except one surface with a solution of 5% (w/v) cellulose acetate and 1% (w/v) dibutyl phthalate. Different permeation enhancers like 2% sodium deoxycholate, 2% sodium cholate hydrate (SCH) and 5% menthol were tested. Swelling index, ex vivo residence time, mucoadhesion strength, in vivo testing of mucoadhesion time, in vitro dissolution and ex vivo permeation were carried out. Furthermore, compatibility and accelerated stability studies were performed for the drug excipients. Finally, drug bioavailability of the BH.2HCl-optimized buccal mucoadhesive formulation was compared with that of the orally administered Betaserc® 24 mg tablet in six healthy male volunteers.ResultsFormulation F10, which contained a combination of 35% guar gum and 5% sodium carboxymethyl cellulose, exhibited long adhesion time, high adhesion strength and diminished irritation to volunteers and showed zero-order release kinetics. SCH produced a significant enhancement in permeation of BH.2HCl across buccal mucosa. BH.2HCl-optimized buccal mucoadhesive formulation showed percentage relative bioavailability of 177%.ConclusionThe developed mucoadhesive tablets represent a promising alternative for the buccal delivery of BH.2HCl.

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Section: Resultsmentioning

confidence: 96%

Section: Resultsmentioning

confidence: 99%

Transbuccal delivery of betahistine dihydrochloride from mucoadhesive tablets with a unidirectional drug flow: in vitro, ex vivo and in vivo evaluation

El-Nabarawi¹,

Ali²,

Aboud³

et al. 2016

DDDT

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“…After an equilibration time with PBS for 30 minutes, the permeability experiments were started by replacing the media in a receiver chamber with 8 mL fresh PBS pH 7.4 (37°C) and that of the donor chamber with 100 µL (equivalent to 0.032 mg of TA) of each of the tested formulations. 15 At predetermined time intervals (2, 4, 6, 8, and 24 hours), the entire receptor medium was withdrawn from the receiver compartment and replenished with an equal volume of fresh PBS at 37°C. Samples from the receptor media were filtered through the 0.45-µm Millipore filter analyzed for TA using the HPLC (PerkinElmer Inc.).…”

Section: Ex Vivo Bovine Nasal Mucosal Retentionmentioning

confidence: 99%

Rationally designed nanocarriers for intranasal therapy of allergic rhinitis: influence of carrier type on in vivo nasal deposition

Sallam

Helal

Mortada

2016

IJN

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The aim of this study is to develop a locally acting nasal delivery system of triamcinolone acetonide (TA) for the maintenance therapy of allergic rhinitis. The effect of encapsulating TA in different nanocarriers on its mucosal permeation and retention as well as in vivo nasal deposition has been studied. A comparative study was established between polymeric oil core nanocapsules (NCs), lipid nanocarriers such as nanoemulsion (NE), and nanostructured lipid carriers (NLCs). The elaborated nanocarriers were compared with TA suspension and the commercially available suspension “Nasacort ® ”. The study revealed that NC provided the highest mucosal retention, as 46.14%±0.048% of the TA initial dose was retained after 24 hours, while showing the least permeation through the nasal mucosa. On the other hand, for TA suspension and Nasacort ® , the mucosal retention did not exceed 23.5%±0.047% of the initial dose after 24 hours. For NE and NLC, values of mucosal retention were 19.4%±0.041% and 10.97%±0.13%, respectively. NC also showed lower mucosal irritation and superior stability compared with NE. The in vivo nasal deposition study demonstrated that NC maintained drug in its site of action (nasal cavity mucosa) for the longest period of time. The elaborated polymeric oil core NCs are efficient carriers for the administration of nasally acting TA as it produced the least permeation results, thus decreasing systemic absorption of TA. Although NCs have been administered via various routes, this is the first study to implement the polymeric oil core NC as an efficient carrier for localized nasal drug delivery.

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“…(Initial concentration of LFD in the nanoemulgel as well as in ordinary gel in the donor compartment was 10 mg and the effective surface area for permeation was 3.14 cm 2 ). and also on the viscoelastic nature of the gel (Huang et al, 2007 and Steady state diffusion coefficient (D) were calculated using 462 following equations (Pund et al, 2013) and the observations are 463 listed in Table 1. (Boyd, 2012;Kaltwasser, 2007).…”

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confidence: 99%

“…LFD and co-solvents (ethanol, polyethylene glycol 400, propylene 108 glycol and Trancutol P) using shake flask method. An excess of LFD 109 (about 1 g) was added to 1 mL of above mentioned vehicles and the Apparent permeability coefficient (P app , cm À2 min À1 ) and Steady 233 state diffusion coefficient (D) were calculated (Pund et al, 2013). …”

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confidence: 99%

Transcutaneous delivery of leflunomide nanoemulgel: Mechanistic investigation into physicomechanical characteristics, in vitro anti-psoriatic and anti-melanoma activity

Pund¹,

Pawar²,

Gangurde³

et al. 2015

International Journal of Pharmaceutics

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Ex vivo permeation characteristics of venlafaxine through sheep nasal mucosa

Cited by 98 publications

References 29 publications

Transbuccal delivery of betahistine dihydrochloride from mucoadhesive tablets with a unidirectional drug flow: in vitro, ex vivo and in vivo evaluation

Transbuccal delivery of betahistine dihydrochloride from mucoadhesive tablets with a unidirectional drug flow: in vitro, ex vivo and in vivo evaluation

Rationally designed nanocarriers for intranasal therapy of allergic rhinitis: influence of carrier type on in vivo nasal deposition

Transcutaneous delivery of leflunomide nanoemulgel: Mechanistic investigation into physicomechanical characteristics, in vitro anti-psoriatic and anti-melanoma activity

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