Design and in Vitro Characterization of Mucoadhesive Buccal Patches of Duloxetine Hydrochloride

Peddapalli, Himabindu; Chinnala, Krishna Mohan; Banala, Nagaraj

doi:10.22159/ijpps.2017v9i2.13793

Cited by 9 publications

(9 citation statements)

References 23 publications

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“…In a previous study, Peddapalli et al. ( 2017 ) prepared DH buccal patches to improve the drug bioavailability by bypassing the hepatic metabolism and acid degradation in the stomach. This study concluded that DH can be delivered via the buccal route, however, the study did not support this claim by performing pharmacokinetic studies in human subjects.…”

Section: Introductionmentioning

confidence: 99%

Formulation and optimization of duloxetine hydrochloride buccal films: in vitro and in vivo evaluation

2017

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Duloxetine hydrochloride (DH) is a serotonin-norepinephrine reuptake inhibitor (SSNRI) indicated for the treatment of depression. Duloxetine suffers from reduced oral bioavailability (≈50%) due to hepatic metabolism. This study aims to develop DH buccoadhesive films to improve its bioavailability. DH buccoadhesive films were prepared adopting the solvent casting method using hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA). The prepared films were evaluated for weight uniformity, drug content, surface pH, swelling index, mucoadhesion strength and drug release percentages. Accelerated stability and bioavailability studies in healthy human volunteers were also performed for the selected films. Results of the evaluation tests showed that the optimum physicochemical characters were obtained by the films prepared with 2% HPMC using 10% propylene glycol (F2 films). Accelerated stability studies revealed that DH showed proved stability throughout the experiment time. DH bioavailability from F2 films was determined and compared with that of the marketed oral capsules (Cymbalta 30 mg). The pharmacokinetic results showed that C for F2 was higher than the market product. In addition, ANOVA analysis showed that a T of F2 film was significantly lower, while, the AUC of F2 was significantly higher than that of Cymbalta capsules. The percentage relative bioavailability of DH from F2 was found to be 296.39%. Therefore, the prepared buccal films offer an alternative route for the administration of DH with the possibility of improving its bioavailability.

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Section: Introductionmentioning

confidence: 99%

Formulation and optimization of duloxetine hydrochloride buccal films: in vitro and in vivo evaluation

2017

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“…When the PVA-PVP layer is placed in contact with the mucosa, the drug compound migrates through the polymer and partitions across the interface of polymer/mucosa, which consequently migrates into the mucosa. The initial fast permeation may be attributed to the rapid diffusion of the drug to the surface of the film [16]. With time, swelling of polymer matrix occurred and varied the entanglement of polymeric pathways to control the drug diffusion from the matrix.…”

Section: In Vitro Permeationmentioning

confidence: 99%

“…Materials with hydrophobicity, low water permeability and drug impermeability properties such as melted wax [10], ethyl cellulose [1,4,11], and Eudragit RL100 [12] have been used as a backing membrane. A wide range of polymers such as hydroxypropyl methylcellulose, carbopol, poly (vinyl alcohol) (PVA), and poly (vinyl pyrrolidone) (PVP) [13][14][15][16][17] have been employed as a matrix and mucoadhesive layer in buccal patches. In order to improve the film properties, including film-forming ability, mechanical and mucoadhesive properties, a combination of hydrophilic polymers is generally used.…”

Section: Introductionmentioning

confidence: 99%

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Preparation and Characterization of Poly (Vinyl Alcohol)–poly (Vinyl Pyrrolidone) Mucoadhesive Buccal Patches for Delivery of Lidocaine HCL

Jaipakdee

Limpongsa

2018

Int J App Pharm

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Objective: The objectives of this study were to prepare and characterize a buccal mucoadhesive patch using poly (vinyl alcohol) (PVA), poly (vinyl pyrrolidone) (PVP) as a mucoadhesive matrix, Eudragit S100 as a backing layer, and lidocaine HCl as a model drug.Methods: Lidocaine HCl buccal patches were prepared using double casting technique. Molecular interactions in the polymer matrices were studied using attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry. Mechanical and mucoadhesive properties were measured using texture analyzer. In vitro permeation of lidocaine HCl from the patch was conducted using Franz diffusion cell.Results: Both of the free and lidocaine HCl patches were smooth and transparent, with good flexibility and strength. ATR-FTIR, DSC and X-ray diffractometry studies confirmed the interaction of PVA and PVP. Mechanical properties of matrices containing 60% PVP were significantly lower than those containing 20% PVP (*P<0.05). Mucoadhesive properties had a tendency to decrease with the concentration of PVP in the patch. The patch containing 60% PVP had significantly lower muco-adhesiveness than those containing 20% PVP (*P<0.05). In vitro permeation revealed that the pattern of lidocaine HCl permeation started with an initial fast permeation, followed by a slower permeation rate. The initial permeation fluxes follow the zero-order model of which rate was not affected by the PVP concentrations in the PVA/PVP matrix. Conclusion:Mucoadhesive buccal patches fabricated with PVA/PVP were successfully prepared. Incorporation of PVP in PVA/PVP matrix affected the strength of polymeric matrix and mucoadhesive property of patches.

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“…Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation, a drug administered through the buccal mucosa enters directly the systemic circulation, thereby minimizing the firstpass hepatic metabolism and adverse gastrointestinal effect [6]. The oral mucosa, mainly the buccal site rather attractive for drug delivery [7], because the mucosa is relatively permeable with a rich blood supply, it is easily accessible, relatively immobile mucosa, suitable for administration of retentive dosage forms, termination of therapy at any time, comparatively less susceptibility to enzymatic activity, and useful for pediatric and geriatric patients. Hence, various mucoadhesive dosage forms were prepared for oral delivery, in the form of adhesive tablets [8][9][10][11][12][13], adhesive gels, buccal ointments [14,15], Bioadhesive Wafers [16], Bioadhesive lozenges [17], Bioadhesive Microparticles [18], and adhesive patches [19,20].…”

Section: Introductionmentioning

confidence: 99%

Formulation, in Vitro and Ex Vivo Characterization of Mucoadhesive Buccal Tablets for Antihypertensive Drug

Peddapalli

Bakshi

Boggula

2018

Asian J Pharm Clin Res

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Objective: Olmesartan belongs to a class of angiotensin II receptor blockers. It is used in the treatment of hypertension. However, it undergoes extensive hepatic first-pass metabolism, resulting in low oral bioavailability is about 26%. The aim of this study was to prepare and evaluate the mucoadhesive buccal tablets of olmesartan with a goal to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal tablets were prepared by a direct compression technique using mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC K4M), sodium carboxymethylcellulose (SCMC), and Carbopol 934P. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, ex vivo mucoadhesive strength, ex vivo mucoadhesive time, and ex vivo permeation studies. The release kinetics was calculated to determine the drug release mechanism. Results: The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets F2, F7, and F11 showed satisfactory drug release rates with the diffusion controlled mechanism. Optimized buccal tablets developed for olmesartan possess reasonable mucoadhesive strength, mucoadhesive time, and surface pH was in an acceptable salivary pH 6.76±0.28–6.89±0.34. The ex vivo permeation studies for optimized tablets were shown satisfactory drug permeation and could meet the target flux 0.991 mg h−1cm−2.Conclusion: The obtained results could be used as a platform to develop the buccal delivery of this drug, which bypasses the first-pass metabolism and results in the improvement of bioavailability. Hence, the present study concludes that the olmesartan could be delivered through the buccal route.

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Design and in Vitro Characterization of Mucoadhesive Buccal Patches of Duloxetine Hydrochloride

Cited by 9 publications

References 23 publications

Formulation and optimization of duloxetine hydrochloride buccal films: in vitro and in vivo evaluation

Formulation and optimization of duloxetine hydrochloride buccal films: in vitro and in vivo evaluation

Preparation and Characterization of Poly (Vinyl Alcohol)–poly (Vinyl Pyrrolidone) Mucoadhesive Buccal Patches for Delivery of Lidocaine HCL

Formulation, in Vitro and Ex Vivo Characterization of Mucoadhesive Buccal Tablets for Antihypertensive Drug

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