Flexible New Dosage Forms Containing Carvedilol for the Treatment of Patients with Cardiovascular Disorders: Development, Stability, Palatability, and Microbiological Studies.

The development of formulations adapted to the patient's age is a challenge in the pharmaceutical industry. Pediatric and geriatric patients may have difficulties in swallowing oral medications when an adequate formulation is not available. Carvedilol is a poorly water-soluble drug used to treat cardiovascular problems; it is commercialized in several countries only as solid oral formulations, which are often manipulated at the point of administration to treat pediatric or geriatric patients.

Miconazole Nitrate Microparticles in Lidocaine Loaded Films as a Treatment for Oropharyngeal Candidiasis.

Oral candidiasis is an opportunistic infection that affects mainly individuals with weakened immune system. Devices used in the oral area to treat this condition include buccal films, which present advantages over both oral tablets and gels. Since candidiasis causes pain, burning, and itching, the purpose of this work was to develop buccal films loaded with both lidocaine (anesthetic) and miconazole nitrate (MN, antifungal) to treat this pathology topically.

The Effect of Different Formulations of Praziquantel in Reducing Worms in the Prepatent Period of Schistosomiasis in Murine Models.

Schistosomiasis is a widely distributed parasitic disease and one of the most important neglected tropical diseases globally, for which Praziquantel® (PZQ) is the only available treatment. In this context, tests with new PZQ formulations become relevant for disease control. This study evaluated the effects of PZQ treatment in the prepatent phase of schistosomiasis using two formulations: nanoencapsulated (PZQ-NANO) and active pharmaceutical ingredient (PZQ-API).

Design and optimization of pH-sensitive Eudragit nanoparticles for improved oral delivery of triclabendazole.

Design of Experiments (DoE) techniques were used to identify and optimize the parameters involved in the formulation of triclabendazole pH-sensitive Eudragit® nanoparticles (NPs). Using a Placket Burmann design, Eudragit® E, Eudragit® RS, and two stabilizers (PVP and PVA) were evaluated for NPs formulation by nanoprecipitation. Based on the screening results, Eudragit E 100® and PVP were selected as excipients, and their levels were studied and optimized using a central composite design, obtaining an optimum nanoparticulated system with a Size of 240 nm, a PDI of 0.

Effect of sex and genotype of the host on the anthelmintic efficacy of albendazole microcrystals, in the CBi-IGE infection murine model.

Albendazole (ABZ) is an anthelmintic pharmaceutical commonly used in the treatment of nematode infections. It is a Class II drug poorly water-soluble, with very low bioavailability, a feature particularly limiting to treat the trichinellosis chronic phase. Microcrystals obtained by controlled precipitation using hydroxyethyl cellulose and chitosan have previously been shown to improve ABZ biopharmaceutical properties.

Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization.

A new tioconazole (TCZ) mucoadhesive film, based on a biodegradable chitosan/ hydroxypropyl methylcellulose (CH/HPMC) blend, was developed for treatment of vaginal candidiasis. The formulation was optimized through an I-optimal design (minimizing the integral of the prediction variance across the factor space), where the impact of the proportion of the ingredients and processing variables on the quality of the final product was evaluated. Both, the thickness of the film and the swelling index, which affect patients' comfort and compliance, were considered.

Orphan Formulations for Pediatric Use: Development and Stability Control of Two Sildenafil Citrate Solutions for the Treatment of Pulmonary Hypertension.

Sildenafil citrate causes vasodilatation, relaxation of the smooth muscle, and reduction of pulmonary arterial pressure. The latter property makes sildenafil citrate efficient for the treatment of cardiovascular diseases, including pulmonary arterial hypertension. Pediatric patients with pulmonary arterial hypertension are more susceptible to errors in drug administration than adults because of a lack of suitable drug dosages.

Nanodelivery of nitazoxanide: impact on the metabolism of cysticerci intracranially inoculated in mice.

To formulate nanocapsules and nanoemulsions of nitazoxanide (NTZ) and evaluate the metabolic effect on cysticerci inoculated intracranially into mice. NTZ nanosystems were formulated through solvent diffusion methodology. These nanoformulations were administered perorally and their impact on glycolysis, the tricarboxylic acid cycle and fatty acid metabolism in cysticerci was investigated.

Effect of Genotype and Sex of the Host on the Bioavailability of Novel Albendazole Microcrystals Based on Chitosan and Cellulose Derivatives.

Albendazole (ABZ), an anthelmintic compound widely used in the treatment of systemic nematode infections, is included in the list of class II drugs based on the Biopharmaceutical Classification System. ABZ has limited effectiveness due to its poor water solubility and consequent low bioavailability. Bioavailability of novel ABZ microcrystals based on hydroxyethylcellulose (S4A) or chitosan (S10A) was studied in male and female mice of two inbred lines, from the murine CBi-IGE model of trichinellosis, differing in susceptibility to this parasitosis (line CBi/L, resistant; line CBi+, susceptible).

A Novel Prototype Device for Microencapsulation of Benznidazole: In Vitro/In Vivo Studies.

This study was aimed to design a simple and novel prototype device for the production of polymeric microparticles. To prove the effectiveness of this device, benznidazole microparticles using chitosan as carrier and NaOH, KOH, or SLS as counter ions were used. For comparison, benznidazole microparticles were prepared by the conventional dripping technique (syringe and gauge) using the same excipients.

Preparation, Physicochemical Characterization and In Vitro and In Vivo Activity Against Heligmosomoides polygyrus of Novel Oral Formulations of Albendazole and Mebendazole.

Albendazole (ABZ) and mebendazole (MBZ) are the 2 most commonly used drugs in the treatment of soil-transmitted helminth infections in humans, but their performance is hampered by low solubility and physicochemical properties. We developed different formulations (β-cyclodextrin inclusion complexes, chitosan-based microcrystals (CH), and polyvinyl alcohol and polysorbate 80-based nanoparticles [P80]) of ABZ and MBZ with an improved in vitro solubility profile and tested their activities in vitro and in vivo against the hookworm Heligmosomoides polygyrus. We found that all formulations tested showed a faster and higher dissolution level and were more active than the standard drugs.

Improving the Dissolution of Triclabendazole from Stable Crystalline Solid Dispersions Formulated for Oral Delivery.

Triclabendazole belongs to the class II/IV of the Biopharmaceuticals Classification System, and its low aqueous solubility represents a major drawback during the development of effective dosage forms. Therefore, the goal of this study was to elucidate whether polymeric solid dispersions would represent a suitable approach to overcome such disadvantage. Due to the lack of information on triclabendazole release, four different dissolution media were evaluated to analyze drug dissolution rate.

Design and Characterization of Chitosan Nanoformulations for the Delivery of Antifungal Agents.

Among different Candida species triggering vaginal candidiasis, is the most predominant yeast. It is commonly treated using azole drugs such as Tioconazole (TIO) and Econazole (ECO). However, their low water solubility may affect their therapeutic efficiency.

New approaches to identification and characterization of tioconazole in raw material and in pharmaceutical dosage forms.

Tioconazole (TCZ), a broad-spectrum antifungal agent, has significant activity against and other species, and therefore, it is indicated for the topical treatment of superficial mycoses. The main goal of this work is to report an exhaustive identification and characterization procedure to improve and facilitate the online quality control and continuous process monitoring of TCZ in bulk material and loaded in two different dosage forms: ovules and nail lacquer. The methodologies were based on thermal (differential scanning calorimetry (DSC), melting point, and thermogravimetry (TG)), spectroscopic (ultraviolet (UV), Raman, near infrared (NIR), infrared spectroscopy coupled to attenuated total reflectance (FTIR-ATR), and nuclear magnetic resonance (NMR)), microscopic and X-ray diffraction (XRD).

Chitosan-hydroxypropyl methylcellulose tioconazole films: A promising alternative dosage form for the treatment of vaginal candidiasis.

Vaginal candidiasis is considered a frequent opportunistic mucosal infection and the second most common cause of vaginitis after bacterial vaginosis. In this work, different vaginal films based on chitosan, hydroxypropyl methylcellulose and blends of these polymers containing tioconazole, were developed and thoroughly characterized to improve the conventional therapeutics of vaginal candidiasis. Mechanical properties, swelling, adhesiveness, morphology, antifungal activity, hemocompatibility and cytotoxicity were evaluated.

Chitosan-based nanodelivery systems applied to the development of novel triclabendazole formulations.

Triclabendazole is a poorly-water soluble (0.24 μg/mL) compound classified into the Class II/IV of the Biopharmaceutical Classification System. It is the drug of choice to treat fascioliasis, a neglected parasitic disease worldwide disseminated.

Repositioning of Anti-parasitic Drugs in Cyclodextrin Inclusion Complexes for Treatment of Triple-Negative Breast Cancer.

Drug repositioning refers to the identification of new therapeutic indications for drugs already approved. Albendazole and ricobendazole have been used as anti-parasitic drugs for many years; their therapeutic action is based on the inhibition of microtubule formation. Therefore, the study of their properties as antitumor compounds and the design of an appropriate formulation for cancer therapy is an interesting issue to investigate.

Solving the Delivery Problems of Triclabendazole Using Cyclodextrins.

Triclabendazole is the first-line drug of choice to treat and control fasciolasis, a neglected parasitic human disease. It is a class II/IV compound according to the Biopharmaceutics Classification System. Thus, the aim of this study was to improve aqueous solubility and dissolution rate of triclabendazole complexed with 2-hydroxylpropyl-β-cyclodextrin (HP-β-CD) and methyl-β-cyclodextrin (Me-β-CD) at 1:1 and 1:2 M ratio.

Correction to: First Development, Optimization, and Stability Control of a Pediatric Oral Atenolol Formulation.

In the INTRODUCTION section, Atenolol is defined in parenthesis as (ATN, Fig. 1.) The correct definition is (ATN).

First Development, Optimization, and Stability Control of a Pediatric Oral Atenolol Formulation.

Liquid formulations can be used in children of different ages by varying the volume of the administered dose in order to ensure an exact dosage. The aim of this work was to develop and to optimize a safe liquid atenolol formulation and to carry out the corresponding chemical and microbiological stability studies. A Plackett-Burman design was used to determine the factors that could be critical in the development of the formulations, and a central composite design was used to determine the optimal working conditions.

Structural Elucidation of Poloxamer 237 and Poloxamer 237/Praziquantel Solid Dispersions: Impact of Poly(Vinylpyrrolidone) over Drug Recrystallization and Dissolution.

Praziquantel (PZQ) is the recommended, effective, and safe treatment against all forms of schistosomiasis. Solid dispersions (SDs) in water-soluble polymers have been reported to increase solubility and bioavailability of poorly water-soluble drugs like PZQ, generally due to the amorphous form stabilization. In this work, poloxamer (PLX) 237 and poly(vinylpyrrolidone) (PVP) K30 were evaluated as potential carriers to revert PZQ crystallization.

Application of Fluorescence Emission for Characterization of Albendazole and Ricobendazole Micellar Systems: Elucidation of the Molecular Mechanism of Drug Solubilization Process.

Albendazole (ABZ) and ricobendazole (RBZ) are referred to as class II compounds in the Biopharmaceutical Classification System. These drugs exhibit poor solubility, which profoundly affects their oral bioavailability. Micellar systems are excellent pharmaceutical tools to enhance solubilization and absorption of poorly soluble compounds.

Development and in vitro/in vivo evaluation of a novel benznidazole liquid dosage form using a quality-by-design approach.

Objectives: To develop an alcohol-free solution suitable for children of benznidazole, the drug of choice for treatment of Chagas disease.

Methods: In a quality-by-design approach, a systematic optimisation procedure was carried out to estimate the values of the factors leading to the maximum drug concentration. The formulations were analysed in terms of chemical and physical stability and drug content.

Development and Evaluation of Buccal Films Based on Chitosan for the Potential Treatment of Oral Candidiasis.

In this work, chitosan films were prepared by a casting/solvent evaporation methodology using pectin or hydroxypropylmethyl cellulose to form polymeric matrices. Miconazole nitrate, as a model drug, was loaded into such formulations. These polymeric films were characterized in terms of mechanical properties, adhesiveness, and swelling as well as drug release.