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Pharmaceutical Development and Technology

Eric Lambert, Jelena M Janjic
Multiple linear regression (MLR) modeling as a novel methodological advancement for design, development and optimization of perfluorocarbon nanoemulsions (PFC NEs) is presented. The goal of the presented work is to develop MLR methods applicable to design, development and optimization of PFC NEs in broad range of biomedical uses. Depending on the intended use of PFC NEs as either therapeutics or diagnostics, nanoemulsion composition differs in respect to specific applications (e.g. magnetic resonance imaging, drug delivery, etc)...
February 6, 2019: Pharmaceutical Development and Technology
Gamal Mohamed Mahrous, Mohamed Abbas Ibrahim, Haitham Fady Mostafa, Ehab Mostafa Elzayat
Orally dissolving tablets (ODTs) represent one of the recent advances in drug delivery. The foremost objective of this study was to optimize the utilization of lubricant sodium stearyl fumarate in the preparation of dextromehorphan hydrobromide ODTs with enhanced taste-masking properties. Simple blending of sodium stearyl fumarate with the powder bed would result in taste-masking through physical adsorption of the lubricant particles on the drug particles. A randomized 32 full factorial experimental design was used to characterize the relationship between lubricant ratio (X1), mixing time (X2), and the tablet properties...
February 4, 2019: Pharmaceutical Development and Technology
Dherya Bahl, Saloni Daftardar, Rinda Devi Bachu, Sai Hs Boddu, Nezam Altorok, Bashar Kahaleh
Asbtract The purpose of this work was to design and characterize a topical formulation of econazole nitrate (EN) with potential for treating Raynaud's phenomenon (RP). Four topical dosage forms (F1_topical solution, F2_HPMC or hydroxypropyl methylcellulose dispersion, F3_ VersaBase® cream and F4_ Lipoderm® Activemax™ Cream) containing 3% w/w EN were prepared and characterized for drug content, pH, viscosity, spreadability, drug crystallinity, stability and in vitro permeation using Franz cells across pig ear skin, and results were compared to the 1% marketed EN cream...
February 4, 2019: Pharmaceutical Development and Technology
Dana Kawar, Hamdy Abdelkader
Since FDA approval of the first transdermal patch in 1979, the utilizing of skin as a route of systemic drug administration has attracted the attention of the formulation scientists. The liposomes research in the area of transdermal drug delivery has been around for decades. This study aimed at comparing the latest gel-core liposomes (hyaluosomes) with non-conventional liposomal systems such as propylene glycol (PG)-liposomes, ethosomes, transferosomes and conventional liposomes loaded with ketoprofen. The modified thin film hydration method was used to prepare these liposomal systems; size, zeta potential, EE%, TEM, rheological properties, in-vitro release and ex-vivo permeation studies were performed...
January 24, 2019: Pharmaceutical Development and Technology
Ramin Sakhtianchi, Behrad Darvishi, Zahra Mirzaie, Farid Dorkoosh, Saeed Shanehsazzadeh, Rassoul Dinarvand
Fulfilling the purpose of developing a NP with theragnostic capabilities, the current study describes synthesis of an aptamer-functionalized PEG-coated SPION/mesoporous silica core-shell nanoparticle for concurrent cancer targeted therapy and magnetic resonance imaging. SPIONs were synthesized according to a thermal decomposition method and served as cores for SPION/mesoporous silica core/shell nanoparticles (MMSNs). Doxorubicin was then successfully loaded in MMSNs which were then coated with di-carboxylic acid functionalized poly ethylene glycol (PEG-MMSNs)...
January 18, 2019: Pharmaceutical Development and Technology
Nussana Thitichai, Chalaisorn Thanapongpibul, Man Theerasilp, Witaya Sungkarat, Norased Nasongkla
The present study examined the cytotoxicity and magnetic resonance imaging (MRI) distribution of cancer-targeted, MRI-visible polymeric micelles that encapsulate doxorubicin (DOX) and superparamagnetic iron oxide (SPIO) and are conjugated with glucose as a targeting ligand. In this study, the micelles were characterized by dynamic light scattering to determine particle size and zeta potential. Morphology and structure of the micelles were evaluated by transmission electron microscopy. To investigate the clinical potential of glucose-micelles, in vitro cytotoxicity assays of nonencapsulating or SPIO-and-DOX-coencapsulating micelles were performed on L929 mouse fibroblasts, and we found that glucose-micelles did not exert in vitro cytotoxic effects...
January 17, 2019: Pharmaceutical Development and Technology
Clare Frances Rawlinson Malone, Ana Patricia Ferreira, Daniel Nicholls, Sarah Nicholson
Amorphous spray dried dispersions (SDDs) are a key enabling technology for oral solid dosage formulations, used to improve dissolution behaviour and clinical exposure of poorly-soluble active pharmaceutical ingredients (APIs). Appropriate assessment of amorphous dissolution mechanisms is an ongoing challenge. Here we outline the novel application using Focused Beam Reflectance Measurement (FBRM) to analyse particle populations orthogonal to USP 2 dissolution. The relative impact of polymer substitution and particle attributes on 25% BMS-708163/HPMC-AS SDD dissolution was assessed...
January 14, 2019: Pharmaceutical Development and Technology
Upendra Bulbake, Nagavendra Kommineni, Maksim Ionov, Maria Bryszewska, Wahid Khan
Delivery of negatively charged, high molecular weight and unstable siRNA is difficult. The present study describes the development and comparison of cationic liposomes (CLs) and polyamidoamine (PAMAM) dendrimer generation 4 (PG4) nanocarriers of gene for cancer therapy. CLs and PG4 were complexed with anticancer siRNA (siPlk1) to form siPlk1-CLs lipoplex and siPlk1-PG4 dendriplex. siPlk1-CLs/PG4 complexes were characterized for average particle size, zeta potential, fluorescence and integrity of siPlk1 by agarose gel electrophoresis, ethidium bromide intercalation assay, circular dichroism, protection against RNase and stability in serum...
January 11, 2019: Pharmaceutical Development and Technology
Masatoshi Honjo, Okuhara Yasuhide, Masayoshi Yamada, Sei Higuchi, Kenji Mishima, Sharmin Tanjina, Taku Michael Aida, Takafumi Kato, Makoto Misumi, Tadashi Suetsugu, Hideaki Orii, Keiichi Irie, Kazunori Sano, Kenichi Mishima, Tomomitsu Satho, Takunori Harada
The work reported here is an extension of our previous findings in which supercritical composite particles (SCP) of alpha lipoic acid (ALA) masked with hydrogenated colza oil (HCO) named as ALA/HCO/SCP were obtained by the modified particles from gas-saturated solutions (PGSS) process in supercritical carbon dioxide in order to obscure the unpleasant taste and odor of ALA. The masking effect on ALA/HCO/SCP was compared with the widely used mechano-chemiclally masked formulation of ALA and HCO named as MC-50F...
January 11, 2019: Pharmaceutical Development and Technology
Nozad Hussein, Huner Omer, Ava Ismael, Mohamed Albed Alhnan, Abdelbary Elhissi, Waqar Ahmed
Ropinirole hydrochloride (RH) is an anti-Parkinson drug with relativity low oral bioavailability owing to its extensive hepatic first pass metabolism. Spray-dried mucoadhesive alginate microspheres of RH were developed and characterized followed by histopathological evaluation using nasal tissue isolated from sheep. Spherical microparticles having high product yield (around 70%) were obtained when the inlet temperature of spray drying was 140 °C. Fourier Transform Infrared (FTIR) studies revealed the compatibility of the drug with the polymer, and scanning electron microscopy (SEM) showed that drug-loaded microparticles were spherical, and the apparent surface roughness was inversely related to the ratio of polymer to drug...
January 10, 2019: Pharmaceutical Development and Technology
Xiaomei Su, Danshen Zhang, Haiwei Zhang, Kaiyan Zhao, Wenshu Hou
The purpose of this work was to prepare and characterize Angiopep-2 functionalized ginsenoside-Rg3 loaded nanoparticles (ANG-Rg3-NP) and evaluate the therapeutic effect on C6 glioma cells. Nanoparticles were prepared by the emulsion solvent evaporation method. Angiopep-2 was functionalized to nanoparticles via a maleimide-thiol covalent binding reaction to obtain ANG-Rg3-NP. The prepared nanoparticles were evaluated for size, zeta potential, morphology, stability, encapsulation efficiency, loading capacity and release properties...
January 2, 2019: Pharmaceutical Development and Technology
Lijun Zhen, Qiuyu Wei, Qilong Wang, Huiyun Zhang, Michael Adu-Frimpong, Caleb Kesse Firempong, Ximing Xu, Jiangnan Yu
6-Gingerol, an active herbal ingredient of ginger, has various bioactivities such as anti-neurodegenerative disease, anti-inflammatory and so on. The aim of the present study was to enhance the oral bioavailability and brain distribution of 6-Gingerol via polymeric micelles. A polymeric micelles drug delivery system of 6-Gingerol consisting of D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and Poly (ethylene glycol)-poly (ε-caprolactone) (PEG-PCL) was prepared via solvent injection method. The developed 6-Gingerol-loaded TPGS/PEG-PCL micelles (6-GTPMs) were characterized based on particle size, polydispersity index (PDI), Zeta potential, encapsulation efficiency (EE), drug loading (DL) and in vitro release profile...
December 17, 2018: Pharmaceutical Development and Technology
Samer R Abulateefeh, Ghada K Al-Adhami, Mahmoud Y Alkawareek, Alaaldin M Alkilany
The ability to control the internal core architecture of polymeric microcapsules has a direct impact on their applications. However, this task, especially to produce microcapsules with a high percentage of mononuclear aqueous cores, proved to be challenging. In this work, and in continuation to our previous studies, we report a facile protocol to prepare poly(D,L-lactide-co-glycolide) (PLGA) microcapsules with unprecedented percentage (almost 100%) of mononuclear aqueous cores by the internal phase separation method via adding alcohols...
December 17, 2018: Pharmaceutical Development and Technology
Sirima Soodvilai, Wajee Tipparos, Worranan Rangsimawong, Prasopchai Patrojanasophon, Sunhapas Soodvilai, Warayuth Sajomsang, Praneet Opanasopit
This research aimed to evaluate the effects of silymarin (SM)-loaded polymeric micelles (PMs) on the renal toxicity and anticancer activity of cisplatin. Amphiphilic chitosan derivatives were employed to develop SM-loaded PMs. The permeation across an intestinal membrane, cytotoxicity, and renal toxicity of cisplatin during the treatment were evaluated. The SM-loaded PMs had small particle sizes (326-336 nm), negative surface charge, high entrapment efficiency (47-70%), and demonstrated pH-sensitive release...
December 7, 2018: Pharmaceutical Development and Technology
Mostafa Zamani, Amin Shirinzadeh, Mozhgan Aghajanzadeh, Sina Andalib, Hossein Danafar
PURPOSE: In this study, methoxy poly (ethylene glycol) -poly (ε-caprolactone) (mPEG-PCL) di block copolymers were synthesized. The purpose of this work is to investigate the in vivo anti-inflammatory effects of simvastatin-loaded micelles. METHODS: The structure of synthesized copolymers were characterized by using HNMR, FTIR and GPC techniques. Simvastatin was encapsulated in micelles through a single-step nano-precipitation method, leading to formation of simvastatin-loaded mPEG-PCL (simvastatin-mPEG-PCL) micelles...
December 5, 2018: Pharmaceutical Development and Technology
Joana R Campos, Ana R Fernandes, Raquel Sousa, Joana F Fangueiro, Prapaporn Boonme, Maria Luisa Garcia, Beatriz C Naveros, Eliana B Souto
The aim of this work has been the development of a non-toxic, long-term stable solid lipid nanoparticles (SLN) formulation for the loading of Nimsulide (NiM) by a 22 factorial design. The optimized formulation was composed of 10 wt% of glyceryl behenate and 2.5 wt% of poloxamer 188. Immediately after production, Z-Ave of NiM-SLN was 166.1 ± 0.114 nm, with a polydispersity index (PI) of 0.171 ± 0051 and zeta potential nearly neutral (-3.10 ± 0.166 mV). A slight increase of Z-Ave was recorded for NiM-SLN stored at 25 °C for a period of 15 days, whereas at 4 °C particles kept size within similar range...
November 26, 2018: Pharmaceutical Development and Technology
Ibrahim El-Serafi, Orlaith Loy, Ying Zhao, Sandra Oerther, Jonas Mattsson
INTRODUCTION: Treosulfan is an alkylating agent that is used for the treatment of ovarian cancer and for conditioning prior to stem cell transplantation. It is a prodrug that is activated non-enzymatically to two active epoxides. OBJECTIVES: To optimize a protocol for both in vivo samples handling and in vitro drug preparation. Treosulfan stability was tested in biological fluids at different conditions as well as for its cytotoxicity on cell lines. RESULTS: Plasma samples can be safely frozen for a short period up to 8h, however; for longer periods, samples should be acidified...
November 26, 2018: Pharmaceutical Development and Technology
Misbah Tabbassum, Farrukh Zeeshan
This study was conducted to investigate the influence of formulation development methods on the stability (secondary structure, aggregation and biological activity) of protein drugs embedded in lipid matrices. Catalase, horseradish peroxidase and α-chymotrypsin were employed as model proteins while, Precirol® AT05 (glyceryl palmitostearate) was used as lipid matrix. Protein loaded lipid matrices were prepared using melting and mixing and wet granulation methods. Attenuated total reflectance Fourier transform infrared (ATR FT-IR) spectroscopy, size exclusion chromatography (SEC) and biological activity analyses were performed...
November 26, 2018: Pharmaceutical Development and Technology
Bashar Alkhalidi, Hatim S AlKhatib, Mohammad Saleh, Saja Hamed, Yasser Bustanji, Nader Al Bujuq, Naji Najib, Susana Torrado-Susana, Al-Sayed Sallam
Clarithromycin laurate (CLM-L), a fatty acid salt of clarithromycin (CLM), was prepared by a simple co-melting process. The formation of CLM-L was confirmed using FTIR, 1 H NMR, and 13 C NMR. Solubility, intrinsic dissolution rate (IDR), and partitioning properties of CLM-L were determined and compared to those of CLM. As expected, CLM-L showed a greater hydrophobicity than CLM with lower aqueous solubility, higher partitioning coefficient, and slower dissolution rate in comparison to CLM. Tablets of CLM-L also showed a significantly slower in vitro release in comparison to CLM tablets...
November 25, 2018: Pharmaceutical Development and Technology
Mohammad Mehdi Mahboobian, Ali Seyfoddin, Reza Aboofazeli, Seyed Mohsen Foroutan, Ilva Dana Rupenthal
The aim of this study was to investigate the corneal penetration of brinzolamide nanoemulsions and evaluate their in vitro and ex vivo irritancy potential. Twelve brinzolamide nanoemulsions were prepared by the spontaneous emulsification method and ex vivo permeability studies were conducted using excised bovine corneas fixed onto Franz diffusion cells. To confirm the safety of the formulations for ophthalmic use, preparations were examined for potential ocular irritancy using a cell viability assay on retinal cells, the hen's egg test-chorioallantoic membrane (HET-CAM) and the bovine corneal opacity-permeability (BCOP) test...
November 24, 2018: Pharmaceutical Development and Technology
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