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Jyoti Bhandari, Harshita Mishra, Pawan Kumar Mishra, Rupert Wimmer, Farhan J Ahmad, Sushama Talegaonkar
Cellulose nanofiber (CNF) aerogels with favorable floatability and mucoadhesive properties prepared by the freeze-drying method have been introduced as new possible carriers for oral controlled drug delivery system. Bendamustine hydrochloride is considered as the model drug. Drug loading was carried out by the physical adsorption method, and optimization of drug-loaded formulation was done using central composite design. A very lightweight-aerogel-with-matrix system was produced with drug loading of 18.98%±1...
2017: International Journal of Nanomedicine
Arpa Petchsomrit, Namfa Sermkaew, Ruedeekorn Wiwattanapatapee
Alginate-based composite sponges were developed as carriers to prolong the gastric retention time and controlled release of curcumin-loaded self-microemulsifying drug delivery systems (Cur-SMEDDS). Liquid Cur-SMEDDS was incorporated into a solution made up of a mixture of polymers and converted into a solid form by freeze-drying. The ratio of alginate as the main polymer, adsorbent (colloidal silicon dioxide), and additional polymers-sodium carboxymethyl cellulose (SCMC), hydroxypropyl methylcellulose (HPMC)-was varied systematically to adjust the drug loading and entrapment efficiency, sponge buoyancy, and the release profile of Cur-SMEDDS...
March 15, 2017: Scientia Pharmaceutica
Abeer Khattab, Nashwah Zaki
The purpose of our investigation was to develop and optimize the drug entrapment efficiency and bioadhesion properties of mucoadhesive chitosan microspheres containing ranitidine HCl prepared by an ionotropic gelation method as a gastroretentive delivery system; thus, we improved their protective and therapeutic gastric effects in an ulcer model. A 3 × 2(2) full factorial design was adopted to study the effect of three different factors, i.e., the type of polymer at three levels (chitosan, chitosan/hydroxypropylmethylcellulose, and chitosan/methylcellulose), the type of solvent at two levels (acetic acid and lactic acid), and the type of chitosan at two levels (low molecular weight (LMW) and high molecular weight (HMW))...
March 7, 2017: AAPS PharmSciTech
Anh Q Vo, Xin Feng, Manjeet Pimparade, Xinyou Ye, Dong Wuk Kim, Scott T Martin, Michael A Repka
In the present study, we aimed to prepare a gastroretentive drug delivery system that would be both highly resistant to gastric emptying via multiple mechanisms and would also potentially induce in situ supersaturation. The bioadhesive floating pellets, loaded with an amorphous solid dispersion, were prepared in a single step of hot-melt extrusion technology. Hydroxypropyl cellulose (Klucel™ MF) and hypromellose (Benecel™ K15M) were used as matrix-forming polymers, and felodipine was used as the model drug...
February 28, 2017: European Journal of Pharmaceutical Sciences
Nilesh Desai, Ravindra Purohit
Clopidogrel bisulfate (CBS) is antiplatelet drug and it is becoming a drug of choice in the treatment and management of prevention of heart attacks and strokes. CBS is stable and soluble in acidic pH; therefore, retention in stomach for prolonged period appears to be beneficial for controlling the bioavailability. The gastroretentive osmotic system (GROS) facilitates prolonged retention of drug in stomach and provides zero-order drug release. A complex formulation like GROS poses many challenges, and QbD tools can help in designing robust formulation which takes all aspects of product and process development in order to deliver a robust product...
February 28, 2017: AAPS PharmSciTech
Kyu-Mok Hwang, Cheol-Hee Cho, Nguyen-Thach Tung, Ju-Young Kim, Yun-Seok Rhee, Eun-Seok Park
This study focuses on developing a highly porous floating tablet containing cilostazol. The underlying release mechanism of cilostazol from porous and floating tablets in dissolution media containing surfactants was investigated. The tablets were prepared by compressing granules and excipients with a sublimating agent, followed by sublimation under vacuum. The volatile material for the sublimating agent was chosen based on its flow properties using conventional methods as well as the twisted blade method. Resultant tablets could float immediately and had significantly higher tensile strengths than conventional tablets of similar porosities, holding a promising potential for increasing gastroretentive properties...
February 20, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Smita Raghuvanshi, Kamla Pathak
INTRODUCTION: The study was aimed at the development of low-density gastroretentive bioadhesive microsponges of cinnarizine by two-pronged approach (i) coating with bioadhesive material and (ii) exploration of acconon MC 8-2 EP/NF as bioadhesive raw material for fabrication. MATERIALS AND METHODS: Microsponges were prepared by quasi-emulsion solvent diffusion method using 3(2) factorial design. Capmul GMO was employed for bioadhesive coating. In parallel, potential of acconon for the fabrication of bioadhesive floating microsponges (A8) was assessed...
October 2016: International Journal of Pharmaceutical Investigation
Mahboubeh Razavi, Hamed Karimian, Chai Hong Yeong, Mehran Fadaeinasab, Si Lay Khaing, Lip Yong Chung, Didi Erwandi B Mohamad Haron, Mohamed Ibrahim Noordin
This study aimed to formulate floating gastroretentive tablets containing metformin hydrochloric acid (HCl), using various grades of hydrogel such as tamarind powders and xanthan to overcome short gastric residence time of the conventional dosage forms. Different concentrations of the hydrogels were tested to determine the formulation that could provide a sustained release of 12 h. Eleven formulations with different ratios of tamarind seed powder/tamarind kernel powder (TKP):xanthan were prepared. The physical parameters were observed, and in vitro drug-release studies of the prepared formulations were carried out...
2017: Drug Design, Development and Therapy
Jaber Emami, Mahboubeh Rezazadeh
BACKGROUND: A very simple, sensitive, and accurate high-performance liquid chromatography (HPLC) method with ultraviolet detector was developed and applied to determine ciprofloxacin in human plasma following administration of a gastroretentive formulation developed in our laboratory. MATERIALS AND METHODS: HPLC analysis was performed on a C18 μ-Bondapack column (250 mm × 3.9 mm) using acetonitrile: potassium dihydrogen phosphate solution 0.1 M (20:80, v/v, pH 3) at a flow rate of 1...
2016: Advanced Biomedical Research
Priya Vashisth, Navdeep Raghuwanshi, Amit Kumar Srivastava, Harmeet Singh, Hemant Nagar, Vikas Pruthi
The purpose of this investigation is to formulate a gastroretentive sustained drug release system for ofloxacin to improve its retention time, pharmacological activity, bioavailability and therapeutic efficacy in the stomach. Ofloxacin loaded gellan/poly vinyl alcohol (PVA) nanofibers were fabricated using a simple and versatile electrospinning technique. The fabricated nanofibers were evaluated for percent drug encapsulation efficiency and in vitro drug release in simulated gastric medium (pH1.2). The in vitro release profile and kinetic studies for drug indicated the sustained release of ofloxacin from the nanofibers through Fickian diffusion kinetics...
February 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
Debjani Sarkar, Gouranga Nandi, Abhijit Changder, Prasenjit Hudati, Sayani Sarkar, Lakshmi Kanta Ghosh
Development of a gastroretentive sustained release tablet of metformin based on poly (acrylic acid)-grafted-gellan (PAAc-g-GG) is the main purpose of this study. At first, PAAc-g-GG was synthesized by microwave-promoted free radical initiation method using cerric (IV) ammonium nitrate (CAN) as redox initiator and characterized by elemental analysis, FTIR, DSC-TGA, (13)C NMR, biodegradation and viscosity study. The synthetic parameters were optimized by 2(3) full factorial design using Design Expert software...
March 2017: International Journal of Biological Macromolecules
Maria Eliza Freitas, Marta Ruiz-Lopez, Susan H Fox
Levodopa remains the most effective treatment for Parkinson's disease and is considered the gold standard therapy. However, disease progression and changes in the gastrointestinal tract result in a declining window of treatment response in a majority of patients. Efforts have been made recently to improve levodopa bioavailability either by developing more effective oral formulations or by innovating routes of administration (intestinal infusion, transcutaneous or inhaled levodopa). IPX066 is a novel levodopa-carbidopa (LD/CD) oral formulation combining immediate-release (IR) and extended-release (ER) LD/CD recently approved in the USA and the EU...
November 2016: CNS Drugs
Kyu-Mok Hwang, Woojin Byun, Cheol-Hee Cho, Eun-Seok Park
The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion-spheronization and sublimation under vacuum. Granules prepared with sublimation at 60°C displayed a slower dissolution rate and smoother surface morphology than those prepared at lower temperatures. This was unexpected as the reported melting point of glyceryl behenate is higher than 69°C...
October 10, 2016: Pharmaceutical Development and Technology
Md Lutful Amin, Tajnin Ahmed, Md Abdul Mannan
PURPOSE: The purpose of this study was to develop and evaluate metronidazole loaded floating-mucoadhesive microsphere for sustained drug release at the gastric mucosa. METHODS: Alginate gastroretentive microspheres containing metronidazole were prepared by ionic gelation method using sodium bicarbonate as gas forming agent, guar gum as mucoadhesive polymer, and Eudragit L100 as drug release modifier. Carbopol was used for increasing the bead strength. The microspheres were characterized by scanning electron microscopy and evaluated by means of drug entrapment efficiency, in vitro buoyancy, and swelling studies...
June 2016: Advanced Pharmaceutical Bulletin
A G Mirani, S P Patankar, V J Kadam
The research envisioned was the development of diltiazem hydrochloride effervescent floating matrix tablet using a risk-based approach. Preliminarily, the in vitro drug release profile was derived which theoretically simulated the in vivo condition after oral administration. Considering this as a rationale, the formulation development was initiated with defining the quality target product profile (QTPP) and critical quality attributes (CQAs). The preliminary studies were conducted to screen material attributes and process parameters followed by their risk assessment studies to select the plausible factors affecting the drug product CQAs, i...
October 2016: Drug Delivery and Translational Research
Jeong Soo Kim, Kwang Ho Cha, Seung Yeob Kang, Donghan Won, Sun Woo Jang, Miwon Son, Moon Ho Son, Ho Jung Choi, Young Won Lee, Myung Joo Kang
OBJECTIVE: DA-9601, an extract of Artemisia asiatica containing eupatilin and jaceosidin as active compounds, has been prescribed to treat gastritis in Asia. In recent times, sustained-release, floating gastroretentive (GR) tablets of DA-9601 are available on the market. In the present study, the physical properties and in vitro drug release profile, in vivo gastric residence time, and gastroprotective effect of GR tablet were compared to those of immediate release (IR) tablets of DA-9601...
2016: Drug Design, Development and Therapy
Carla M Lopes, Catarina Bettencourt, Alessandra Rossi, Francesca Buttini, Pedro Barata
In recent decades, many efforts have been made in order to improve drug bioavailability after oral administration. Gastroretentive drug delivery systems are a good example; they emerged to enhance the bioavailability and effectiveness of drugs with a narrow absorption window in the upper gastrointestinal tract and/or to promote local activity in the stomach and duodenum. Several strategies are used to increase the gastric residence time, namely bioadhesive or mucoadhesive systems, expandable systems, high-density systems, floating systems, superporous hydrogels and magnetic systems...
August 20, 2016: International Journal of Pharmaceutics
Yu Huang, Yumeng Wei, Hongru Yang, Chao Pi, Hao Liu, Yun Ye, Ling Zhao
5-Fluorouracil (5-FU) was loaded in hollow microspheres to improve its oral bioavailability. 5-FU hollow microspheres were developed by a solvent diffusion-evaporation method. The effect of Span 80 concentration, ether/ethanol volume ratio, and polyvinyl pyrrolidone/ethyl cellulose weight ratio on physicochemical characteristics, floating, and in vitro release behaviors of 5-FU hollow microspheres was investigated and optimized. The formulation and technology composed of Span 80 (1.5%, w/v), ether/ethanol (1...
2016: Drug Design, Development and Therapy
Neel Mehta, Iwona Bucior, Shay Bujanover, Rajiv Shah, Amitabh Gulati
BACKGROUND: Postherpetic neuralgia (PHN) interferes with patients' quality of life, and disturbed sleep is a prevalent complaint. Pain-associated sleep interference in turn enhances pain and/or reduces pain tolerance. Therefore, reducing sleep interference by pain, in addition to pain control, may improve patient care. To address this notion, we characterized relationships among changes in pain intensity, sleep interference, and overall impression of improvement in PHN patients treated with gastroretentive gabapentin (G-GR)...
April 1, 2016: Health and Quality of Life Outcomes
Shweta Agarwal, R S R Murthy
Mucoadhesive tablets have emerged as potential candidates for gastroretentive drug delivery providing controlled release along with prolonged gastric residence time. Gastroretentive mucoadhesive tablets could result in increased bioavailability due to prolonged gastric residence time. A hydrophilic matrix system was developed as mucoadhesion is achievable on appropriate wetting and swelling of the polymers used. The polymers were so chosen so as to provide a balance between swelling, mucoadhesion and drug release...
November 2015: Indian Journal of Pharmaceutical Sciences
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