Fluconazole Mucoadhesive Buccal Films: In Vitro/In Vivo Performance

Yehia, Soad A.; El‐Gazayerly, Omaima N.; Basalious, Emad B.

doi:10.2174/156720109787048195

Cited by 90 publications

(54 citation statements)

References 17 publications

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“…Films have traditionally been found to be safe in humans for oral and vaginal use. They are used to orally deliver pain medications, vitamins, and supplements (65)(66)(67). Microbicide drugs, such as dapivirine, retrocyclin-101, cellulose acetate phthalate, and dapivirine in combination with TFV, have been formulated into films for vaginal use, and VCF containing nonoxynol-9, a VCF lubricating film, and a vaginal cleansing film (Apothecus Pharmaceuticals) are all available commercially (25,(28)(29)(30)(31)(32).…”

Section: Discussionmentioning

confidence: 99%

“…Low residence time has been reported with traditional vaginal dosage forms, such as suppositories and liquid formulations, due to the self-cleaning action of the vaginal tract (73,74). The bioadhesive properties of films may increase the local retention time and improve clinical performance (65)(66)(67). The median vaginal fluid concentrations of IQP-0528 obtained 60 min after film application were 3 log greater than the in vitro IC 90 of 0.146 g/ml (45), with a time to maximum concentration of drug in serum (T max ) of 15,795.08 g/ml at 4 h. The median vaginal fluid level obtained 24 h after application was 3.3 log higher than the in vitro IC 90 (Fig.…”

Section: Discussionmentioning

confidence: 99%

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Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis

Srinivasan

Zhang

Martin

et al. 2016

Antimicrob Agents Chemother

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dFor human immunodeficiency virus (HIV) prevention, microbicides or drugs delivered as quick-dissolving films may be more acceptable to women than gels because of their compact size, minimal waste, lack of an applicator, and easier storage and transport. This has the potential to improve adherence to promising products for preexposure prophylaxis. Vaginal films containing IQP-0528, a nonnucleoside reverse transcriptase inhibitor, were evaluated for their pharmacokinetics in pigtailed macaques. Polymeric films (22 by 44 by 0.1 mm; providing 75% of a human dose) containing IQP-0528 (1.5%, wt/wt) with and without poly(lactic-co-glycolic acid) (PLGA) nanoparticle encapsulation were inserted vaginally into pigtailed macaques in a crossover study design (n ‫؍‬ 6). With unencapsulated drug, the median ( In the absence of an effective vaccine, preexposure prophylaxis (PrEP) with antiretroviral (ARV) drugs is currently a very promising biomedical intervention to control the human immunodeficiency virus (HIV) epidemic (1, 2). PrEP involves the use of ARV by high-risk HIV-negative individuals to prevent HIV acquisition. Many ARVs that have traditionally been used for HIV treatment have advanced as PrEP agents due to their safety and potency profiles (1,(3)(4)(5). Of the available ARVs, tenofovir disoproxil fumarate (TDF), a nucleoside reverse transcriptase inhibitor (NRTI) used widely in HIV treatment, has been studied extensively in animals and humans as a PrEP agent (3, 5). The success with oral TDF and Truvada, TDF in combination with emtricitabine (FTC), in inhibiting HIV infection in nonhuman primates led to the clinical trials in humans with TDF and Truvada (1, 6-11). In stark contrast to the success of TDF and Truvada in clinical trials in men who have sex with men and heterosexual HIV-discordant couples, two large clinical trials in women with oral Truvada, VOICE and FEM-PrEP, have demonstrated no protection due to a lack of adherence (12, 13).Providing optimal dosage forms of potent HIV PrEP agents for women has the potential to improve product adherence (14,15). Topical dosage forms can be effective in reducing HIV infection, as demonstrated by the CAPRISA 004 vaginal 1% tenofovir (TFV) gel trial, where per-protocol use of the gel before and after sex with no more than 2 doses in 24 h (BAT-24) reduced HIV acquisition by 39% (2). As observed in the oral PrEP trials, greater efficacy was reported among the high adherers in CAPRISA 004 (54% versus 28% in the low adherers) (2). Subsequent trials with 1% TFV gel, such as FACTS 001, employing the BAT-24 regimen used in CAPRISA-004, and the VOICE trial, with a daily application of 1% TFV gel, were not effective in protecting women against HIV acquisition (12, 16). It was estimated based on the returned used applicators that only 13% of the FACTS 001 trial participants were able to use the gel in Ն80% of sex acts per month (16). Neither the noncoital daily application of the TFV gel with VOICE nor the pericoital vaginal dosing regimen with FACTS 001 demonstrated effecti...

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis

Srinivasan

Zhang

Martin

et al. 2016

Antimicrob Agents Chemother

View full text Add to dashboard Cite

show abstract

“…(19). In addition, the subsequent increase in the diffusional path length due to the high swelling index may be responsible for the low release profile (31). It was also observed that the addition of Carbopol (F5-F6) led to a decrease in the drug release efficiency significantly (p < 0.05) due to the formation of gelatinous layer upon hydration that protects the film against erosion.…”

Section: Swelling Indexmentioning

confidence: 98%

“…This could be explained on the basis of the degree of erosion of the two polymers, where the increase in SCMC may result in increasing film porosity which facilitates dissolution medium penetration. This would consequently accelerate film erosion and detachment from the mucus membrane (22,31). The mucoadhesion time ranged from 1 to 12 h, according to the composition of the formulation.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Design and In Vitro/In Vivo Evaluation of Ultra-Thin Mucoadhesive Buccal Film Containing Fluticasone Propionate

et al. 2016

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ABSTRACT. Fluticasone propionate is a synthetic corticosteroid drug distinguished by its potent antiinflammatory action with low systemic side effects in comparison to other corticosteroids making it a potential drug for local buccal delivery. The aim of the present study was to design mucoadhesive buccal film containing fluticasone that is aesthetically acceptable and could maintain local drug release for a sustained period to manage the sign and symptoms of severe erosive mouth lesions. Solvent casting technique was used in film preparation. Different polymeric blends were used either alone or in combination with mucoadhesive polymers, sodium carboxymethyl cellulose (SCMC), or Carbopol 971P at different concentrations. The physicochemical properties, in vitro mucoadhesion time as well as the drug release properties for all prepared formulations were determined. Selected formulations with adequate properties were further examined by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) and subjected to in vivo evaluation. Films containing hydroxypropyl methylcellulose (HPMC)/ ethyl cellulose (EC) showed acceptable physicochemical properties, homogenous drug distribution, convenient mucoadhesion time, moderate swelling as well as sustained drug release up to 12 h. The biological performance of these formulations was assessed on healthy human volunteers and compared with a prepared mouthwash which showed enhanced pharmacokinetic parameters for the selected films in comparison to the mouthwash. The results revealed that the optimized formulation containing HPMC/EC and 10% SCMC could successfully achieve sustained drug release for 10 h which is considered promising for local treatment of severe mouth lesions.

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“…Mucoadhesive strength was determined for all the formulations using the modified balance method (Yehia et al, 2009). As shown, the bioadhesive strength of formulations H1 and H2 which contained HPMC and SCMC showed higher value than that of PVA and sodium alginate-contained films (H3 and H4), respectively.…”

Section: In Vitro Mucoadhesion Strengthmentioning

confidence: 99%

Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism

Rana¹,

Murthy²

2013

Drug Delivery

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Context: Mucoadhesive buccal films containing three layers (mucoadhesive layer, nanosuspension containing layer and backing membrane) were incorporated with carvedilol nanosuspension. Objective: Formulation and evaluation of nanosuspension incorporated mucoadhesive buccal films of carvedilol for bioavailability enhancement by avoiding first-pass metabolism. Methods: Carvedilol-loaded nanosuspension was prepared by a precipitation-ultrasonication method with varying concentrations of the polymer. The formulation was analyzed for size, size distribution, surface charge and morphology. Optimized nanosuspension was incorporated into drug gel layer which was sandwiched between a mucoadhesive layer and a backing layer to form tri-layered buccal films. They were evaluated for their physical, mechanical and bioadhesive parameters followed by in vitro and in vivo studies. Results and discussion: Nanosuspension showed a negative zeta potential (À17.21 mV) with a diameter of around 495 nm and a polydispersity index of 0.203. Nanosuspension incorporated drug gel layer (62.4% drug loading) was optimized to contain 3% HPMC and 50 mg Carbopol 934P. The mucoadhesive layer and the backing layer were optimized to contain 3% HPMC and 1% ethyl cellulose, respectively. In vitro drug release was 69% and 62.4% in 9 h across synthetic membrane and porcine buccal mucosa, respectively. In vivo studies conducted in rabbit model showed 916% increase in the relative bioavailability in comparison to marketed oral tablet formulation. The C max and T max of the prepared formulation increased due to increased surface area of drug and also by-passing hepatic metabolism. Conclusion: The drug delivery system has been designed as a novel platform for potential buccal delivery of drugs having high first-pass metabolism.

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Fluconazole Mucoadhesive Buccal Films: In Vitro/In Vivo Performance

Cited by 90 publications

References 17 publications

Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis

Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis

Design and In Vitro/In Vivo Evaluation of Ultra-Thin Mucoadhesive Buccal Film Containing Fluticasone Propionate

Formulation and evaluation of mucoadhesive buccal films impregnated with carvedilol nanosuspension: a potential approach for delivery of drugs having high first-pass metabolism

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