04. September 2018
A decrease in the release rate over time is typically encountered when dealing with hydrophilic matrix systems for oral prolonged release due to progressive increase of the distance the drugmolecules have to cover to diffuse outwards and reduction of the area of the glassy matrix at the swelling front. In order to solve this issue, a novel formulation approach based on non-uniformdistribution of the active ingredient throughout the swellable polymer matrix was proposed and evaluated. Various...
31. August 2018
Combined micro- and nanosystems are appealing for pulmonary protein delivery, fulfilling the specific physiological requirements for efficient outcomes in-vivo. However, fabrication of protein formulations may impose stresses perturbing protein conformational stability and, hence, biological activity. Herein, a protein, insulin (INS), was nanoencapsulated inside chitosan nanoparticles (CS NPs) by ionic gelation. By spray drying, the resultant protein-loaded NPs were further encapsulated with a...
26. August 2018
The aim of this study was to develop roflumilast dry powder inhaler (DPI) formulations by spray drying using hydroxypropyl-β-cyclodextrin (HPβCD) and to determine their suitability for pulmonary delivery. Different feed solution concentrations, solvent systems and spray drying parameters were used to obtain the formulations which were characterized using X-ray powder diffraction, thermal analysis, scanning electron microscopy, particle size distribution, bulk and tapped density, specific...
20. August 2018
Material properties are known to have a significant impact on pharmaceutical manufacturing performance, particularly for solid product processes. Evaluating the performance of a specific material, for example an active pharmaceutical ingredient or excipient, is critical during development stages in order to determine the impact of material properties on the process. However, materials may be scarce during the early stages of process development due to high cost, unavailability, import...
30. July 2018
The number of biologics in the therapeutic development pipeline is increasing including those delivered though inhalation (Morales, 2017; Fathe, 2016). Biologics comprise a broad variety of complex macromolecules with unique physicochemical characteristics. These distinctive characteristics control their pharmacological mechanisms of action, stability, and ultimately affect their processing, formulation, and delivery requirements. This review systematically covers crucial aspects of biologic...
07. July 2018
The pulmonary route of administration has been commonly used for local lung conditions such as asthma and chronic obstructive pulmonary disease (COPD). Recently, with the advent of new technologies available for both formulation and device design, molecules usually delivered at high doses, such as antibiotics and insulin to treat cystic fibrosis (CF) and diabetes, respectively, can now be delivered by inhalation as a dry powder. These molecules are generally delivered in milligrams instead of...
29. May 2018
Powder flow is critical to the success of various pharmaceutical processes such as tableting and capsule filling. Despite a plethora of flow characterisation techniques and parameters available, powder flow still remains to be a not well understood subject. Inter-relationships between the various powder flow parameters in particular have not been well established. Furthermore, while it is known that particle size and shape are important determinants of powder flow, their relative impact on...
27. May 2018
A systematic assessment of key material attributes of active pharmaceutical ingredients (APIs) using minimal material approach is illustrated at the particulate level and bulk level. At a bulk level, flowability improvement of an API through crystal habit manipulation is exemplified. The impact of crystal structures and particulate properties (crystal habit and crystal size) on their mechanical behaviour were addressed by measuring powder tabletability. Bulk powder flow and tabletability were...
23. May 2018
Delivery of drugs to the lungs via dry powder inhaler (DPI) is a promising approach for the treatment of both local pulmonary conditions and systemic diseases. Though DPIs are widely used for the pulmonary deposition of potent bronchodilators, anticholinergics, and corticosteroids, there is growing interest in the utilization of this delivery system for the administration of high drug doses to the lungs, as made evident by recent regulatory approvals for anti-microbial, anti-viral and osmotic...
15. May 2018
Asolventless process for simultaneously milling and dry coating microcrystalline cellulose (MCC) was investigated for producing fine excipients in five different sizes (∼20, 25, 30, 35, 40µm) havinghigh bulk density (BD), good flow function coefficient (FFC), and excellent compaction. Avicel PH-102, used as the starting material, was milled and coated with two grades of silicas, hydrophobic andhydrophilic (R972P and A200), using a fluid energy mill (FEM). Through judicious selection of the...