Chitosan lactate wafer as a platform for the buccal delivery of tizanidine HCl: In vitro and in vivo performance

El-Mahrouk, G. M.; El‐Gazayerly, Omaima N.; Aboelwafa, Ahmed A.; Taha, Maie S.

doi:10.1016/j.ijpharm.2014.03.049

Cited by 53 publications

(20 citation statements)

References 40 publications

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“…The ion spray voltage was adjusted at 3000 V. The common parameters were as follows: nebulizer gas pressure was 45 psi, gas temperature was 275 C and gas flow rate was 8 l/min. The analysis was carried out at the multiple reaction monitoring (MRM) mode, and its MS parameters were as follows: precursor ion (Da) was 254.1 and 326.5 for TIZ and tolterodine, respectively, whereas product ion (Da) was 44.2 and 147.2 for TIZ and tolterodine, respectively (El-Mahrouk et al, 2014).…”

Section: Lc-ms/ms Assay Of Tizmentioning

confidence: 99%

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

2017

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The purpose of the current study was to develop tizanidine HCl (TIZ; a myotonolytic agent used for treatment of spasticity) loaded nanotransfersomes intended for rectal administration, aiming to bypass the hepatic first-pass metabolism. TIZ-loaded nanotransfersomes were prepared by thin-film hydration method followed by characterization for various parameters including entrapment efficiency, vesicle diameter, in vitro release and ex vivo permeation studies. Transfersomal formulation composed of phosphatidylcholine and Tween 80 at a weight ratio of (85:15) gave a satisfactory results. It exhibited encapsulation efficiency of 52.39%, mean diameter of 150.33 nm, controlled drug release over 8 h and good permeation characteristics. Optimum formula was then incorporated into Pluronic-based thermoreversible gel using hydroxypropyl methylcellulose (HPMC) as a mucoadhesive polymer. Pharmacokinetic study was performed by rectal administration of transfersomes-loaded in situ gel to rabbits and compared with oral drug solution and rectal TIZ in situ gel. The pharmacokinetic study revealed that the transfersomal formulation successively enhanced the bioavailability of TIZ by about 2.18-fold and increased t 1/2 to about 10 h as compared to oral solution. It can be concluded that encapsulation of TIZ into nanotransfersomes can achieve a dual purpose of prolonged TIZ release and enhanced bioavailability and so may be considered as a promising drug delivery system for the treatment of spasticity.

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Section: Lc-ms/ms Assay Of Tizmentioning

confidence: 99%

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

2017

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“…PLGA-based wafers, coated with a mucoadhesive layer of starch, NaCMC or Carbopol ® 971P, showed good adhesive properties and were able to release antimicrobial agents with a zero-order release kinetics [159]. Wafers of tizanidine were prepared by incorporation of chitosan lactate beads, cross-linked with sodium tripolyphosphate, into chitosan lactate solution followed by lyophilization [160]. Mucoadhesion to the buccal mucosa was maintained for 8 h without irritation.…”

Section: Wafersmentioning

confidence: 99%

A focus on mucoadhesive polymers and their application in buccal dosage forms

Russo

Selmin

Baldassari

et al. 2016

Journal of Drug Delivery Science and Technology

129

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“…The in vivo mucoadhesive performance test was carried out in three healthy volunteers aged 20–35 years. The buccal tablets (n=3) were adhered, just above the canine tooth, to the gingival mucosa by pressing for 30 s onto mucosa and kept for a period of 16 h 24. The volunteers were claimed to note:

The adhesion time: time required for the tablet to detach from the buccal mucosal surface

The adhesion strength (unadhesive, slightly adhesive, adhesive or very adhesive)

Any irritation signs (non-irritant, slight, moderate or severe)

Bitter taste as a result of BH.2HCl swallowing (non, slight, moderate or very)

The mucoadhesive tablet disintegration in the buccal cavity (non, slight, moderate or high)

…”

Section: Methodsmentioning

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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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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Chitosan lactate wafer as a platform for the buccal delivery of tizanidine HCl: In vitro and in vivo performance

Cited by 53 publications

References 40 publications

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

A focus on mucoadhesive polymers and their application in buccal dosage forms

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

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