Preparation and evaluation of ßcyclodextrin-based nanosponges loaded with Budesonide for pulmonary delivery.

Budesonide (BUD) is a glucocorticosteroid used to treat chronic obstructive pulmonary disease. Despite this, it is a hydrophobic compound with low bioavailability. To address these hurdles, non-toxic and biocompatible ßcyclodextrin-based nanosponges (ßCD-NS) were attempted. BUD was loaded on five different ßCD-NS at four different ratios. NS with 1,1'-carbonyldiimidazole (CDI) as a crosslinking agent, presented a higher encapsulation efficiency ( Ì´ 80%) of BUD at 1:3 BUD: ßCD-NS ratio (BUD-ßCD-NS). The optimized formulations were characterized by Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), water absorption capacity (WAC), scanning electron microscopy (SEM), X-ray powder diffraction studies (XRD), particle size, zeta potential, encapsulation efficiency, in vitro and in vivo release studies, acute toxicity study, solid-state characterization, and aerosol performance. In vitro-in vivo correlation and cytotoxicity of the formulations on alveolar cells in vitro were further determined. In vitro and in vivo studies showed almost complete drug release and drug absorption from the lungs in the initial 2 h for pure BUD, which were sustained up to 12 h from BUD loaded into nanosponges (BUD-ßCD-NS). Acute toxicity studies and in vitro cytotoxicity studies on alveolar cells proved the safety of BUD-ßCD-NS. Several parameters, including particle size, median mass aerodynamic diameter, % fine particle fraction, and % emitted dose, were evaluated for aerosol performance, suggesting the capability of BUD-ßCD-NS to formulate as a dry powder inhaler (DPI) with a suitable diluent. To sum up, this research will offer new insights into the future advancement of ßCD-NS as drug delivery systems for providing controlled release of therapeutic agents against pulmonary disease.

Designing Optimum Drug Delivery Systems Using Machine Learning Approaches: a Prototype Study of Niosomes.

This study demonstrates a machine learning approach in designing optimized drug formulations. Preferred Reporting Items for Systematic Reviews and Meta-Analyses system was adopted to screen literature resulting in 114 niosome formulations. Eleven properties (input parameters) related to drugs and niosomes affecting particle size and drug entrapment (output variables) were precisely identified and used for the network training. The hyperbolic tangent sigmoid transfer function with Levenberg-Marquardt backpropagation was used to train the model. The network showed the highest prediction accuracy of 93.76% and 91.79% for % drug entrapment and particle size prediction. Sensitivity analysis identified drug/lipid ratio and cholesterol/surfactant ratio as the most significant factors affecting % drug entrapment and particle size of niosomes. Accordingly, nine Donepezil hydrochloride noisome batches were prepared using a 3 × 3 factorial design with drug/lipid ratio and cholesterol/surfactant ratio as factors to validate the developed model. The model reached a prediction accuracy of more than 97% for experimental batches. Finally, the superiority of global artificial neural network was demonstrated compared to the local response surface methodology for Donepezil niosome formulations. Even though the ANN successfully predicted the parameters of Donepezil niosomes, several drugs with different physicochemical properties must be tested to confirm the validity of the model and its usefulness for designing new drug niosomal formulations.

Directly compressible medicated chewing gum formulation for quick relief from common cold.

INTRODUCTION: Common cold is the most frequently recurring disease in the world and is a leading cause of doctor visits and missed days from school and work. Cold reliever medicated chewing gum (MCG) will be a definitive patient acceptable solution for this condition. Anti-allergic, cetirizine (CTZ) is a BCS class-I (highly soluble and highly permeable) non-sedating antihistaminic drug and this study was based on the hypothesis that CTZ as a BCS class I drug will be easily released from chewing gum into the salivary fluid within few minutes of chewing and can be easily permeated from oral mucosa by the pressure created by the chewing action and absorbed to a larger extent into the systemic circulation. Therefore, ultimately patients will get quick relief from symptoms of common cold with greater compliance compared to other conventional dosage forms. MATERIALS AND METHODS: This study mainly focuses on taste masking of CTZ by inclusion complexation method, its formulation development in the MCG form and its quality and performance evaluation with the study of potential factors affecting drug release by 3(2) full factorial experimental design. A "chew out" study is carried out to assess in vivo drug release from MCG, in which residual amount is extracted from the chewed sample. RESULTS: Formulation ingredients, such as elastomers, softeners, bulking agents, play an important role in the feel of the final product and its consistency; while sweeteners and flavors play a very essential character in its sensory properties. CONCLUSION: Interindividual variation in chewing frequency and chewing intensity is the main factor which affects release of active ingredient from MCG; while salivary dilution and involuntary swallowing are main reasons for variability in the absorption site, i.e., either from buccal mucosa or from gastrointestinal tract.

Medicated chewing gum--a potential drug delivery system.

IMPORTANCE OF THE FIELD: Over the years, patient convenience and patient compliance-orientated research in the field of drug delivery has resulted in bringing out potential innovative drug delivery options. Out of which, medicated chewing gum (MCG) offers a highly convenient patient-compliant way of dosing medications, not only for special population groups with swallowing difficulties such as children and the elderly, but also for the general population, including the young generation. AREAS COVERED IN THIS REVIEW: In this review, various formulation ingredients, different manufacturing processes, and assessment of in vivo and in vitro drug release from MCG are thoroughly discussed along with the therapeutic potential and limitations of MCG. WHAT THE READER WILL GAIN: Readers will gain knowledge about the rationale and prominent formulation and performance evaluation strategies behind chewing gum as a drug delivery system. TAKE HOME MESSAGE: The availability of directly compressible co-processed gum material enables rapid, safe and low-cost development of MCG as a drug delivery option. By MCG formulation, revitalization of old products and reformulation of new patented products is possible, to differentiate them from upcoming generics competition in the market.

A review on mouth dissolving films.

The ultimate goal of any drug delivery system is the successful delivery of the drug to the body; however, patient compliance must not be overlooked. Fast dissolving drug delivery systems, such as, Mouth Dissolving Films (MDF), offer a convenient way of dosing medications, not only to special population groups with swallowing difficulties such as children and the elderly, but also to the general population. MDF are the novel dosage forms that disintegrate and dissolve within the oral cavity. Intra-oral absorption permits rapid onset of action and helps by-pass first-pass effects, thereby reducing the unit dose required to produce desired therapeutic effect. The present review provides an overview of various polymers that can be employed in the manufacture of MDF and highlights the effect of polymers and plasticizers on various physico-mechanical properties of MDF. It further gives a brief account of formulation of MDF and problems faced during its manufacture.

Multifunctional coprocessed excipients for improved tabletting performance.

With the advancement of tablet manufacturing process, the demand of excipients with improved functionalities, mainly in terms of flow and compression properties, has increased. Coprocessed excipients are a mixture of two or more existing excipients at subparticle level, offer substantial benefits of the incorporated excipients and minimize their drawbacks. These multipurpose excipients have dramatically reduced the number of incorporating excipients in the tablet. The present review discusses the potential advantages of coprocessing and coprocessed excipients, material characteristics required for coprocessing, methods of coprocessing and various coprocessed excipients for direct compression available in the market.