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...
29. March 2018
Docetaxel (DTX) is a chemotherapy drug that can be used for different type of cancers. Due to polysorbate 80, the excipient in the formulation, acute hypertensivity reaction is observed after intravenous administration. The development of oral formulation for DTX has always been problematic as the bioavailability of the drug is shown to be low due to P-glycoprotein efflux transporters and the intestinal metabolism by CYP3A4 enzymes. The objective of this study is to develop novel DTX in situ...
11. August 2017
The goal of this study was to test the feasibility to load non-ordered, non-spherical mesoporous silica with the model drug paracetamol, and subsequently coat the loaded particles using one single pilot scale fluid bed system equipped with a Wurster insert. Mesoporous silica particles (Davisil®) with a size ranging from 310 to 500 μm and an average pore diameter of 15 nm were loaded with paracetamol to 18.8% drug content. Subsequently, loaded cores were coated with ethylcellulose to obtain...
08. March 2017
Abstract Moisture activated dry granulation (MADG) method was used to develop IR tablets with cohesive, fluffy and high dose drugs. To evaluate this approach, three drugs: metformin hydrochloride, acetaminophen and ferrous ascorbate were selected as model compound along with three binders: maltodextrin DE16, PVP K 12 and HPC. The granules were generated using MADG method and tablets were prepared using rotary tablet press. The granules and tablets were characterized for particle size analysis,...
22. November 2016
Abstract The oral bioavailability of poorly soluble drugs can be improved by amorphization generated by loading into the pores of mesoporous particles (pore size 2–50 nm). The main mechanisms are increased kinetic saturation solubility and dissolution velocity due to the amorphous drug state and the nano-size of the drug (=increased dissolution pressure). In this study, the maximum achievable drug loading compared to the theoretical drug loading, and the effect of drug loading degree on the...
21. June 2016
Abstract Mucoadhesive microparticles formulated in a capsule and delivered to the gastrointestinal tract might be useful for local drug delivery. However, swelling and agglomeration of hydrophilic polymers in the gastrointestinal milieu can have a negative influence on particle retention of mucoadhesive microparticles. In this work, we investigated the impact of dry-coating with nano-sized hydrophilic fumed silica on dispersibility and particle retention of mucoadhesive microparticles. As a...
07. June 2016
Purpose To investigate if drug solubility in pharmaceutical excipients used in lipid based formulations (LBFs) can be predicted from physicochemical properties. Methods Solubility was measured for 30 structurally diverse drug molecules in soybean oil (SBO, long-chain triglyceride; TGLC), Captex355 (medium-chain triglyceride; TGMC), polysorbate 80 (PS80; surfactant) and PEG400 co-solvent and used as responses during PLS model development. Melting point and calculated molecular descriptors were...
28. April 2016
The goal of this study was to test the feasibility to load non-ordered, non-spherical mesoporous silica with the model drug paracetamol, and subsequently coat the loaded particles using one single pilot scale fluid bed system equipped with a Wurster insert. Mesoporous silica particles (Davisil®) with a size ranging from 310 to 500 μm and an average pore diameter of 15 nm were loaded with paracetamol to 18.8% drug content. Subsequently, loaded cores were coated with ethylcellulose to obtain...
04. March 2016
The main purpose of this study was to increase the solubility of poorly soluble drug by preparing solid dispersions. Nifedipine (poorly water soluble drug), when prepared as solid dispersion showed increased solubility and dissolution rate. Solid dispersions of Nifedipine were prepared by using silsol 6035 as carrier in various proportions 10%, 20% and 30% by solvent loading (solvent droplet addition)method and various grades of silica by co-milling method in ratios of (1:1, 1:2 and 2:1). The...
15. January 2016
A new formulation method for solid dosage forms with drug loadings from 0.65 ± 0.03% to 39 ± 1% (w/w) of acetaminophen (APAP) as a model drug has been presented. The proposed method involves the production of highly-porous lactose with a BET surface area of 20 ± 1 m2/g as an excipient using a templating method and the incorporation of drug into the porous structure by adsorption from a solution of the drug in ethanol. More