02. October 2018
The formulation of amorphous solid dispersions (ASDs) is an effective way to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The combination of an amorphous state of the drug and the presence of crystallization-inhibiting polymers retains a high amount of dissolved API over time. ASDs with ketoconazole and different polymers were manufactured by spray drying and their characteristics as well as performance were analyzed. Dissolution tests with a...
26. September 2018
The increasing number of poorly water-soluble drug candidates in pharmaceutical development is a major challenge. Enabling techniques such as amorphization of the crystalline drug can result in supersaturation with respect to the thermodynamically most stable form of the drug, thereby possibly increasing its bioavailability after oral administration. The ease with which such crystalline drugs can be amorphized is known as their glass forming ability (GFA) and is commonly described by the...
22. September 2018
Zein is the main storage protein of corn and it has several industrial applications. Mainly in the last 10–15 years, zein has emerged as a potential pharmaceutical excipient with unique features. Zein is a natural, biocompatible and biodegradable material produced from renewable sources. It is insoluble, yet due to its amphiphilic nature, it has self-assembling properties, which have been exploited for the formation of micromicroparticle and nanoparticle and films. Moreover, zein can hydrate...
05. September 2018
The predictability of preformulation screening tools for polymer selection in amorphous solid dispersions (ASD) regarding supersaturation and precipitation was systematically examined. The API-polymer combinations were scaled up by means of hot-melt extrusion and spray-drying to verify the predictions. As there were discrepancies between a solvent-based screening and performance of ASD, a new screening tool with improved predictability at minimal investments of time and material is presented....
16. August 2018
Vaginal drug delivery is a promising route for the treatment and prevention of local and systemic diseases such as genital herpes or AIDS. Suitable excipients must be selected to optimize the residence time of formulations in vaginal mucosa and could be included in the formulation. Many polymers are excellent choices for the development of vaginal drug delivery systems due to their properties of mucoadhesion, biocompatibility and biodegradability. These polymers swell in the aqueous medium of...
14. August 2018
As a relatively new class of materials, single-chain polymer nanoparticles (SCNPs) just entered the field of (biomedical) applications, with recent advances in polymer science enabling the formation of bio-inspired nanosized architectures. Exclusive intramolecular collapse of individual polymer chains results in individual nanoparticles. With sizes an order of magnitude smaller than conventional polymer nanoparticles, SCNPs are in the size regime of many proteins and viruses (1–20 nm)....
13. August 2018
3D printing is an additive manufacturing technique capable of producing various 3D drug products, medical devices, tissues and organs from digital designs. The first FDA approved 3D drug product, Spritam®, has encouraged and attracted many researchers in this field with research undergoing to develop various customized dosage forms. This review aims to introduce 3D printing, its history, advantages, challenges and various techniques used in fabrication of drug products. This review also...
06. June 2018
Hot-melt extrusion is well established in the plastics industry and is applied in pharmaceutical application for more than 30 years. In contrast to plastics, pharmaceutical formulation development is more complex as each formulation is unique in terms of compositions of active pharmaceutical ingredients, carrier and additives. Therefore, new innovative solutions are demanded to tackle the pharma specific challenges in formulation development like how to prevent losses with expensive material...
05. June 2018
Due to the high number of poorly soluble drugs in the development pipeline, novel processes for delivery of these challenging molecules are increasingly in demand. One such emerging method is KinetiSol, which utilizes high shear to produce amorphous solid dispersions. The process has been shown to be amenable to difficult to process active pharmaceutical ingredients with high melting points, poor organic solubility, or sensitivity to heat degradation. Additionally, the process enables classes...
30. May 2018
Blindness and vision impairment are the most devastating global health problems resulting in a substantial economic and social burden. Delivery of drug to particular parts of the anterior or posterior segment has been a major challenge due to various protective barriers and elimination mechanisms associated with the unique anatomical and physiological nature of the ocular system. Drug administration to the eye by conventional delivery systems results in poor ocular bioavailability (< 5%)....