Buccal administration of mucoadhesive blend films saturated with propranolol loaded nanoparticles

Kraisit, Pakorn; Limmatvapirat, Sontaya; Luangtana‐anan, Manee; Sriamornsak, Pornsak

doi:10.1016/j.ajps.2017.07.006

Cited by 70 publications

(39 citation statements)

References 23 publications

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“…Drug dissolution from the ODS involves water diffusion, relaxation of polymer chains, swelling and erosion of the strip . Immediate and fast release of all strips formulae were observed at early time points.…”

Section: Resultsmentioning

confidence: 99%

Reduction of intraocular pressure using timolol orally dissolving strips in the treatment of induced primary open-angle glaucoma in rabbits

El-Feky

Mostafa

Al-Sawahli

et al. 2020

Journal of Pharmacy and Pharmacology

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Objective To enhance bioavailability of timolol (TML) and utilize alternatives for traditional eye drops for more patient compliance, this study was aiming to develop biodegradable orally dissolving strips (ODSs) of TML for treatment of primary open‐angle glaucoma (POAG). Methods Novel ODSs of TML were formulated and optimized using solvent casting method according to full factorial design (31.22). TML ODSs were characterized with respect to many parameters. In‐vivo test was carried out using four groups of 24 New Zealand albino rabbits. POAG was induced by subconjunctival treatment of betamethasone. Histopathological examination and oxidative stress markers assay were carried out. Key findings The optimized formula (F9) exhibited a remarkably 15‐s disintegration time and 96% dissolution rate after 10 min. The results revealed a potent significant inhibitory effect of the optimized TML ODS to reduce IOP in induced rabbits in comparison with control rabbits and TML eye drops‐treated rabbits. The formula showed also high activity against oxidative stress and absence of histopathological changes in iridocorneal angle and cornea. Conclusion The ODSs could be a promising alternative delivery system for eye drops with more compliance to enhance delivery and therapeutic activity of TML in treatment of POAG.

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Section: Resultsmentioning

confidence: 99%

Reduction of intraocular pressure using timolol orally dissolving strips in the treatment of induced primary open-angle glaucoma in rabbits

El-Feky

Mostafa

Al-Sawahli

et al. 2020

Journal of Pharmacy and Pharmacology

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“…The use of nanoparticles as drug carriers is a good strategy to overcome the drawbacks associated with buccal drug delivery. In fact, the nanocarriers may present several advantages such as the increase of the diffusion rate of the drug across the mucus layer, protection of the drug from degradation, and from the drug dilution in the saliva since the nanoparticles adhere to the buccal mucosa prolonging the buccal residence and contact time with the mucosa [48]. In addition, nanocarriers may avoid drug elimination and oral clearance, and have a controlled and/or prolonged drug release profile, resulting in a decreased number of administrations, which improves patient compliance [49].…”

Section: Nanoparticles As Tools For Buccal Drug Deliverymentioning

confidence: 99%

Novel and revisited approaches in nanoparticle systems for buccal drug delivery

Macedo

Castro

Roque

et al. 2020

Journal of Controlled Release

111

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The buccal route is considered patient friendly due to its non-invasive nature and ease of administration. Such delivery route has been used as an alternative for the delivery of drugs that undergo first-pass metabolism or are susceptible to pH and enzymatic degradation, such as occurs in the gastrointestinal tract. However, the drug concentration absorbed in the buccal mucosa is often low to obtain an acceptable therapeutic effect, mainly due to the saliva turnover, tongue and masticatory movements, phonation, enzymatic degradation and lack of epithelium permeation.Therefore, the encapsulation of drugs into nanoparticles is an important strategy to avoid such problems and improve their buccal delivery. Different materials from lipids to natural or synthetic polymers and others have been used to protect and deliver drugs in a sustained, controlled or targeted manner, and enhance their uptake through the buccal mucosa improving their bioavailability and therapeutic outcome. Overall, the main aim of this review is to perform an overview about the nanotechnological approaches developed so far to improve the buccal delivery of drugs. Herein, several types of nanoparticles and delivery strategies are addressed, and a special focus on pipeline products is also given.

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“…HPMC is an extensive hydrophilic polymer used in many pharmaceutical dosage forms, including as a hydrophilic matrix form with prolonged drug release [4,9]. HPMC has many advantages such as ease of use and compression, high levels of drug loading, stability at a wide range of pH, and rapid swelling [4,[9][10][11]. There are several grades of HPMC based on the molecular weight, methoxy group content percentage (-OCH3), and hydroxypropoxy group percentage (-OCH2CH (OH) CH3 6 ) of the molecular structure, resulting in different HPMC viscosities and physical properties [ , 8].…”

Section: Introductionmentioning

confidence: 99%

“…Propranolol hydrochloride (PNL), a β-adrenergic blocking agent, is commonly used for treating hypertension, angina pectoris, and cardiac arrhythmia [2,4,10]. Normally, the conventional tablet form PNL has to be taken three or four daily to maintain drug levels in the bloodstream within the therapeutic range, as its half-life in the circulation is short [10,13]. After oral administration, PNL can be absorbed entirely through the gastrointestinal tract membrane, but only 25-30% bioavailability is achieved due to the hepatic first-pass effect [2,10].…”

Section: Introductionmentioning

confidence: 99%

“…Normally, the conventional tablet form PNL has to be taken three or four daily to maintain drug levels in the bloodstream within the therapeutic range, as its half-life in the circulation is short [10,13]. After oral administration, PNL can be absorbed entirely through the gastrointestinal tract membrane, but only 25-30% bioavailability is achieved due to the hepatic first-pass effect [2,10]. Thus, hydrophilic polymer matrix tablets may be a suitable dosage form for reducing the number of doses taken in one day and helps improve patient compliance.…”

Section: Introductionmentioning

confidence: 99%

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Impact of Hydroxypropyl Methylcellulose (Hpmc) Type and Concentration on the Swelling and Release Properties of Propranolol Hydrochloride Matrix Tablets Usning a Simplex Centroid Design

Kraisit

2019

Int J App Pharm

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Objective: To prepare hydroxypropyl methylcellulose (HPMC) matrix tablets of propranolol hydrochloride (PNL) using a simplex centroid design.Methods: HPMC matrix tablets with different amounts and types of HPMC were prepared by direct compression. A simplex centroid design was used to evaluate tablet weight (1), thickness (Y2), hardness (Y3), axial swelling time at 0.5-12 h (Y4-Y9), radial swelling time at 0.5-12 h (Y10-Y15), and % released at 1-12 h (Y16-Y19). Results:The tablet weight, thickness, and hardness were 397.6-400.4 mg, 3.967-4.029 mm, and 106.9-139.0 N, respectively. The % swelling (axial) and % swelling (radial) Keywords: Hydroxypropyl methylcellulose (HPMC), Matrix tablets, Simplex centroid design, Design of experiment, Propranolol hydrochloride, Swelling, Release mechanism at 0.5-12 h were-8.715 to 59.889 and-1.887 to 49.287, respectively. The negative % swelling could be attributed to erosion of the tablets. The in vitro release of PNL from the tablets in buffer solution pH 1.2 (1 h) and pH 7.5 (3-12 h) was 21.12-76.22%. Tables with a high proportion of K100M HPMC had high PNL release, and the mechanism of PNL release was diffusion-and erosion-controlled. Conclusion:The simplex centroid design is potentially advantageous for formulating PNL-HPMC matrix tablets. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s

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Buccal administration of mucoadhesive blend films saturated with propranolol loaded nanoparticles

Cited by 70 publications

References 23 publications

Reduction of intraocular pressure using timolol orally dissolving strips in the treatment of induced primary open-angle glaucoma in rabbits

Reduction of intraocular pressure using timolol orally dissolving strips in the treatment of induced primary open-angle glaucoma in rabbits

Novel and revisited approaches in nanoparticle systems for buccal drug delivery

Impact of Hydroxypropyl Methylcellulose (Hpmc) Type and Concentration on the Swelling and Release Properties of Propranolol Hydrochloride Matrix Tablets Usning a Simplex Centroid Design

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