Formulation and Characterization of Fast Dissolving films of Etoricoxib

Etoricoxib belongs to a class of drugs called non-steroidal anti-inflammatory drugs (NSAIDs). Etoricoxib acts by reducing the pain and swelling (inflammation) in the joints and muscles of people older than 16 years of age and older patients with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and gout. The present study was aimed to formulate fast dissolving oral films to enhance bioavailability, avoid presystemic metabolism and fast onset of action. The Preformulation studies such as Micromeritics, melting point, partition coefficients, UV spectroscopy, thin layer chromatography, loss on drying were carried out. The fast dissolving oral film was successfully fabricated by solvent casting method. Oral film was fabricated using PVA and PVP polymer. The prepared films were evaluated for Organoleptic evaluations, film weight, thickness, folding endurance, tensile strength, drug content uniformity of films, surface pH, disintegration time and in-vitro dissolution studies and SEM study. The formulation F8 has shown disintegration time of 22±1 seconds and is more promising, showed drug release in phosphate buffer 6.8 pH 86.33% in 10 min. Hence formulation F8 was selected as best formulation. In the stability testing all films stored at elevated temperature showed slight change in pH, other parameters were found to be unchanged.

A REVIEW OF THE COMBINATION OF XANTHINE AND BRONCHODILATOR DRUG IN MOUTH‑DISSOLVING FILM FOR ASTHMA TREATMENT”

There has been an increase in demand for caregiver dosage forms over the past two decades. In the oral cavity, mouth dissolving film dissolves swiftly. Oral films that dissolve in your mouth function best when combined with medications that act quickly, such as Xanthine category drugs (Salbutamol Sulphate) and Xanthene Derivative Theophylline. According to the World Health Organization (WHO), asthma affects one in six adults and a quarter of all children, according to the WHO. A child’s admission to the hospital is often due to asthma, which is one of the most prevalent reasons for admission. During an asthma attack, quick-relief or rescue drugs are used to relax and open the airways, as well as ease symptoms. If prescribed, these medications can also be administered prior to exercise. To treat asthma, a combination of Salbutamol Sulfate and Theophylline is available in tablet form under the brand name “Theo-Asthalin.” Oral films seem to be the most efficacious formulation. As a consequence, children with asthma should receive support from drugs given in the form of mouth-dissolving films, since they provide better patient compliance and an appropriate treatment method.

Mouth Dissolving Film of Domperidone: An approach towards Formulation and its Evaluation

The objective of the current work is to formulate and evaluate the mouth dissolving film of domperidone. It is ideally suitable for the treatment of emesis. The mouth dissolving film of domperidone is useful in the vomiting through the journey. Mouth dissolving films were formulated by the solvent casting technique and its in-vitro as well as the in-vivo evaluation was done by the usual pharmacopoeial and unofficial tests and by using human volunteers. The main benefit of the preparation technique includes fewer operation units, better content consistency. The mouth dissolving film formed was found to be disintegrated in 1 minute. The ratio of components in the aqueous phase affected the thickness, drug content, tensile strength, percentage elongation, folding endurance, and release profile of mouth dissolving film and the best results were obtained for the HPMC E15 and polyethyleneglycol. The compatibility between domperidone and excipients was confirmed by FTIR and DSC studies. The developed mouth dissolving film of domperidone demonstrated usefulness for fast release of drug in mouth, for better drug utilization, and improved patient compliance. The optimized formulation, due to low HPMC E15 content, has optimum tensile strength and thickness. Formulation F8 containing HPMC E15 and PG showed a cumulative % drug release of 95.10 at the end of 12 minutes. HPMC E15 films showed higher cumulative % drug release than films of other HPMC E grades at different concentrations. It was found to be stable during the accelerated stability study. The effect of different concentrations of polymers and plasticizers on in-vitro evaluation parameters was evaluated. Hence, data showed that formulation F8 was the most suitable for the development of fast dissolving oral films of domperidone.

FABRICATION AND CHARACTERIZATION OF FAST DISSOLVING FILMS OF ECLIPTA PROSTRATE LEAVES EXTRACT TO TREAT MOUTH ULCERS

Objective: This research focused on the design of fast dissolving herbal film of Eclipta Prostrate leaves extract for mouth ulcers. Methods: The extract of Eclipta Prostrata leaves was formulated as films by solvent casting method using various polymers viz., HPMC E5, HPMC E15, sodium alginate and PVA. The films were designed by using propylene glycol as a plasticizer, SSG as super disintegrate and honey as a sweetener. Furthermore, the films were evaluated for thickness, folding endurance, weight variation, % elongation, surface pH, % moisture uptake, % moisture loss, disintegration and in vitro drug release study. Results: The revealed that all the films were good in appearance and had a smooth texture. Out of all ten formulations, F3 and F5 disintegrated rapidly with a disintegration time of 27 and 32 seconds. The drug release studies revealed that all the formulations had a good release profile, but the F3 formulation showed rapid release i.e. 83.57% in 4 min. The stability studies revealed that the formulations F3 and F5 were found good with non-tackiness, easily separable and disintegrated at 29 and 33 sec respectively with no appearance and drug release. Conclusion: The research revealed that Eclipta prostrate leaves extract can be formulated into oral films for the treatment of mouth ulcers with improved bioavailability and expected patient compliance.

Phospholipid-containing films for improved drug release

Phospholipids from natural sources can delay liquid-liquid phase separation and improve supersaturation for active pharmaceutical ingredients with poor water-solubility in aqueous media. Researchers have developed oral films containing phospholipids to enhance the dissolution efficiency of hydrophobic pharmaceutical ingredients. Phospholipid-based oral films provide an alternative approach for compounding pharmacies to formulate drugs with poor water solubility.

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75.87 ± 0.55 nm with an average PDI and zeta potential of 0.089 ± 0.01 and 33.5 ± 0.39 mV, respectively. The highest deformability of transfersomes of 18.52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95.15 ± 1.4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174.72 ± 2.3 mg, 0.313 ± 0.03 mm and 36.4 ± 1.1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6.8 ± 0.2 and 10.03 ± 0.4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2.86 folds higher than the pure drug and 1.81 folds higher than plain film (i.e., without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2.95- and 1.7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT.

A comparison between solvent casting and electrospinning methods for the fabrication of neem extract-containing buccal films

In the present study a double layer mucoadhesive buccal film containing nanocarriers encapsulated with neem extract was fabricated through electrospinning and solvent casting techniques for dental therapeutic applications. The morphological, physical and mucoadhesive properties of the resulting electrospun and solvent cast oral films were mutually compared, and their drug release behavior and antibacterial activity were further investigated. Chitosan/poly(vinylalcohol) (PVA) as a mucoadhesive component and phenylalanine amino acid nanotubes (PhNTs)-containing neem extract as a drug nanocarrier were used to fabricate oral films. A poly(caprolactone) (PCL) layer was used as an impermeable backing layer to protect the mucoadhesive component from tongue movement and drug loss. The results indicated an interconnected porous and fully filled solid structures for electrospun and solvent cast films, respectively. The physicomechanical parameters of the samples such as pH, weight, thickness, folding endurance and tensile strength were also evaluated. The crosslinked electrospun buccal film indicated better swelling and mucoadhesive properties compared to the solvent cast film. In addition, the drug loading capacity and encapsulation efficiency of the solvent cast film showed lower experimental values than those of electrospun oral film. On the other hand, the electrospun oral film had a well-controlled release of neem extract up to 82% at oral pH, which is best fitted to the Weibull model, and demonstrated the highest antibacterial properties against S. mutans bacteria with high biocompatibility on L929 fibroblast cells. Generally, the synthesized electrospun mucoadhesive film has a better potential for oral therapeutic applications than the solvent cast film.