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Mucoadhesive microcapsules

Shaheen Sultana, Sushma Talegaonkar, Bhaskar Ray, Harvinder Singh, F J Ahmad, Gaurav Mittal, Aseem Bhatnagar
INTRODUCTION: In this study, different nifedipine-loaded formulations were prepared to treat pylorospasm, a sphincter muscle disorder characterized by delayed gastric emptying process. The efficacy of formulation was evaluated in patients by subjective assessment, gamma scintigraphic approaches, and confocal microscopy. METHODS: Nifedipine-loaded different formulations such as sucrose bead, pellets, and microparticles (slugging method, ionotropic gelation, and chemical denaturation) were designed...
July 2018: Drug Development and Industrial Pharmacy
Paula M Oliveira, Breno N Matos, Priscilla A T Pereira, Taís Gratieri, Lucia H Faccioli, Marcílio S S Cunha-Filho, Guilherme M Gelfuso
Chitosan biocompatibility and mucoadhesiveness make it an ideal polymer for antituberculotic drugs microcapsulation for pulmonary delivery. Yet, previous study indicated toxicity problems to J-774.1-cells treated with some medium molecular weight (190-310kDa) chitosan microparticles. As polymer molecular weight is a crucial factor to be considered, this paper describes the preparation and characterization of chitosan (50-190kDa) microparticles containing isoniazid (INH). Cytotoxicity assays were also performed on murine peritoneal (J-774...
October 15, 2017: Carbohydrate Polymers
Christian Demitri, Leonardo Lamanna, Egidio De Benedetto, Fabrizio Damiano, Maria Stella Cappello, Luisa Siculella, Alessandro Sannino
Alginate micro beads containing Lactobacillus kefiri (the principal bacteria present in the kefir probiotic drink) were produced by a novel technique based on dual aerosols spaying of alginate based solution and CaCl2 as cross linking agent. Carboxymethylcellulose (CMC) has been also added to the alginate in order to change the physic-chemical properties (viscosity and permeability) of the microbeads. Calcium alginate and CMC are biopolymers that can be used for developing oral drug-delivery systems. These biopolymers have been reported to show a pH-dependent swelling behaviour...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
S Swain, A Behera, S C Dinda, C N Patra, Sruti Jammula, S Beg, M E B Rao
The objective of present research work was to design and characterize the venlafaxine HCl-loaded sodium alginate-based mucoadhesive microcapsules by ionic gelation technique using HPMC K100M as mucoadhesive polymer. The Placket-Burman Design was applied for preliminary screening of the formulations and systematic optimization by using Box-Behnken Design. The prepared microcapsules were characterized for drug content, entrapment efficiency, micromeritic properties, particle size, swelling index, mucoadhesive strength, in vitro drug release and in vivo antidepressant activity...
July 2014: Indian Journal of Pharmaceutical Sciences
Alberto Diego-Taboada, Stephen T Beckett, Stephen L Atkin, Grahame Mackenzie
Pollen grain and spore shells are natural microcapsules designed to protect the genetic material of the plant from external damage. The shell is made up of two layers, the inner layer (intine), made largely of cellulose, and the outer layer (exine), composed mainly of sporopollenin. The relative proportion of each varies according to the plant species. The structure of sporopollenin has not been fully characterised but different studies suggest the presence of conjugated phenols, which provide antioxidant properties to the microcapsule and UV (ultraviolet) protection to the material inside it...
2014: Pharmaceutics
Chao Feng, Ruixi Song, Guohui Sun, Ming Kong, Zixian Bao, Yang Li, Xiaojie Cheng, Dongsu Cha, Hyunjin Park, Xiguang Chen
We have designed and evaluated coacervate microcapsules-immobilized multilayer sodium alginate beads (CMs-M-ALG-Beads) for oral drug delivery. The CMs-M-ALG-Beads were prepared by immobilization of doxorubicin hydrochloride (DOX) loaded chitosan/carboxymethyl coacervate microcapsules (DOX:CS/CMCS-CMs) in the core and layers of the multilayer sodium alginate beads. The obtained CMs-M-ALG-beads exhibited layer-by-layer structure and rough surface with many nanoscale particles. The swelling characteristic and drug release results indicated that 4-layer CMs-M-ALG-Beads possessed favorable gastric acid tolerance (the swelling rate <5%, the cumulative drug release rate <3...
March 10, 2014: Biomacromolecules
Shaheen Sultana, Sushama Talegaonkar, Devender Singh, Riyaz Ahmad, Venu Manukonda, Aseem Bhatnagar, F J Ahmad
The present work deals with various attempts to prepare a gastroretentive formulation of lacidipine for treating gastroparesis. High density sucrose beads were modified by coating with certain polymers, but unfortunately sustained release could not be achieved. Granules were prepared by wet granulation technology using different combinations of polymers and a release of the drug was observed. The method failed to release the drug as per desired specifications. Polymeric coating followed by wet granulation was thought to be a better process to sustain the dissolution rate...
July 2013: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Song Chen, Yu Cao, Lynnette R Ferguson, Quan Shu, Sanjay Garg
Probiotic bacteria were previously encapsulated in sub-100 µm Ca(2+) alginate microcapsules for enhanced survival in human gastrointestinal tract. The aim of this study is to evaluate the altered mucoadhesive property of the probiotic delivery system by coating it with mucoadhesive chitosan or thiolated chitosan, for prolonged retention in human colon. The results confirmed that cross-linking with calcium ions reduced the mucoadhesive property of alginate hydrogel, thus questioning the intrinsic mucoadhesiveness of uncoated systems...
2013: Journal of Microencapsulation
Suryakanta Swain, Upali A Behera, Sarwar Beg, J Sruti, Ch Niranjan Patro, S C Dinda, M E B Rao
The objectives of present work was to design and characterize the rabeprazole sodium loaded microcapsules prepared by solvent evaporation technique using ethyl cellulose (EC) based various mucoadhesive polymer, followed by a triple coating with Eudragit L100. The Box-behnken design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The prepared microcapsules were characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity...
April 2013: Drug Development and Industrial Pharmacy
Saahil Arora, R D Budhiraja
Amoxicillin-loaded microcapsules were prepared by ionotropic gelation of sodium alginate (ALG) with chitosan (CS) in presence of calcium chloride as gastroretentive delivery system. The effect of pH, concentration of ALG, CS and calcium chloride, and drug : ALG ratio were optimized in this study for minimizing the degradation of drug in acidic environment and increasing the loading efficacy and mucoadhesive efficiency of microcapsules. The optimum condition for prepared CS-ALG microcapsules was 2%w/v ALG, 0...
January 2012: Journal of Advanced Pharmaceutical Technology & Research
Santhosh Kumar Mankala, Appanna Chowdary Korla, Sammaiah Gade
Microencapsulation is an accepted process used to achieve controlled release and drug targeting for many years. Mucoadhesion has been a topic of interest in the design of drug delivery systems to prolong its intestinal residence time. Mucoadhesion facilitates the intimate contact of the dosage form with the underlying absorption surface for improved bioavailability of drugs. Aceclofenac is a newer nonsteroidal anti-inflammatory drug (NSAID) having short biological half-life of 4-4.3 h, and therefore a sustained release medication is required to get prolonged effect and to reduce fluctuations in drug plasma concentration levels...
October 2011: Journal of Advanced Pharmaceutical Technology & Research
Prabhakar Reddy Veerareddy, Swathi Tedla, Srinivas Reddy Banda, Suresh Bandari, Raju Jukanti
The mucoadhesive microcapsules were prepared by using various concentrations of three different mucoadhesive polymers, namely, chitosan, Carbopol 934P, and methyl cellulose as wall materials and cefdinir as the core material employing orificeionic gelation method. The prepared microcapsules were characterized by scanning electron microscope (SEM) and Fourier transform infrared spectrometry (FT-IR). The prepared microcapsules were found to be spherical with particle size ranging from 765±20 to 985±10 μm and encapsulation efficiencies in the range of 55%-92%...
April 2011: Journal of Advanced Pharmaceutical Technology & Research
Mohammad Ariful Islam, Prati Bajracharya, Sang-Kee Kang, Cheol-Heui Yun, Eun-Mi Kim, Hwan-Jeong Jeong, Yun-Jaie Choi, Eun-Bae Kim, Chong-Su Cho
In this study, thiolated alginate was synthesized by introduction of cysteine to alginate to prepare mucoadhesive alginate/poly (L-lysine)/thiolated alginate (APTA) microcapsules for efficient oral delivery of Lactobacillus salivarius 29 (LS29), a novel therapeutic Lactobacillus strain, in vitro and in vivo. About 759 +/- 32.4 microM of cysteine per gram of alginate was introduced by estimation of Ellman's reagent reaction. LS29-loaded APTA microcapsules provided suitable morphology, size, and a high loading content and efficiency...
August 2011: Journal of Nanoscience and Nanotechnology
Dilipkumar Pal, Amit Kumar Nayak
The purpose of this work was to develop and optimize gliclazide-loaded alginate-methyl cellulose mucoadhesive microcapsules by ionotropic gelation using central composite design. The effect of formulation parameters like polymer blend ratio and cross-linker (CaCl(2)) concentration on properties of gliclazide-loaded alginate-methyl cellulose microcapsules like drug encapsulation efficiency and drug release were optimized. The optimized microcapsules were subjected to swelling, mucoadhesive, and in vivo studies...
December 2011: AAPS PharmSciTech
M A Altaf, Sreedharan, N Charyulu
A new oral drug delivery system was developed utilizing both the concepts of controlled release and mucoadhesiveness, in order to obtain a unique drug delivery system which could remain in stomach and control the drug release for longer period of time. Captopril microcapsules were prepared with a coat consisting of alginate and a mucoadhesive polymer such as hydroxy propyl methyl cellulose, carbopol 934p, chitosan and cellulose acetate phthalate using emulsification ionic gelation process. The resulting microcapsules were discrete, large, spherical and free flowing...
September 2008: Indian Journal of Pharmaceutical Sciences
Hany M Ibrahim, Tarek A Ahmed, Ahmed E A Lila, Ahmed M Samy, Ala A Kaseem, Mohammad T H Nutan
The aim of this project was to develop and optimize indomethacin microcapsules composed of multiple mucoadhesive polymers for high drug entrapment, good mucoadhesiveness and drug release in a controlled fashion over a longer period of time. Microcapsules containing sodium alginate, sodium carboxymethylcellulose, methylcellulose, Carbopol 934 and hydroxypropyl methylcellulose were prepared by orifice-ionic gelation method. The effects of composition of microcapsules on drug entrapment efficacy, drug release and mucoadhesive character were determined by mixture statistical design...
2010: Journal of Microencapsulation
Zeenat Iqbal, Nilu Jain, Gaurav K Jain, Sushama Talegaonkar, Alka Ahuja, Roop K Khar, Farhan J Ahmad
The recognition of periodontal diseases as amenable to local antibiotherapy has resulted in a paradigmatic shift in treatment modalities of dental afflictions. Moreover the presence of antimicrobial resistance, surfacing of untoward reactions owing to systemic consumption of antibiotics has further advocated the use of local delivery of physiologically active substances into the periodontal pocket. While antimicrobials polymerized into acrylic strips, incorporated into biodegradable collagen and hollow permeable cellulose acetate fibers, multiparticulate systems, bio-absorbable dental materials, biodegradable gels/ointments, injectables, mucoadhesive microcapsules and nanospheres will be more amenable for direct placement into the periodontal pockets the lozenges, buccoadhesive tablets, discs or gels could be effectively used to mitigate the overall gingival inflammation...
2008: Recent Patents on Drug Delivery & Formulation
Fei Chen, Yue Zhang, Qiang Liu, Ming-zhi Pang, Xing-gang Yang, Wei-san Pan
A novel mucoadhesive microcapsule with drug-resin complex core loaded with berberine hydrochloride (BH) was developed and optimized. Drug-ion exchange resin (IER) complex was prepared by static method which stirring IER in drug solution at certain conditions. The influences of different IERs, different temperature, pH values and concentrations of drug solution on the drug loading were investigated. IER complex was coated by emulsion-solvent evaporation method. The coating fluid formulation was optimized using central composite design-response surface methodology, where the ratio between Carbopol 934 and IER (X1), the ratio between Eudragit and IER (X2) and the ratio between Eudragit RL and RS (X3) were taken as independent variables...
September 2008: Yao Xue Xue Bao, Acta Pharmaceutica Sinica
S K Prajapati, Purnima Tripathi, Udhumansha Ubaidulla, Vikas Anand
In this study an attempt was made to prepare mucoadhesive microcapsules of gliclazide using various mucoadhesive polymers designed for oral controlled release. Gliclazide microcapsules were prepared using sodium alginate and mucoadhesive polymer such as sodium carboxymethyl cellulose (sodium CMC), carbopol 934P or hydroxy propylmethyl cellulose (HPMC) by orifice-ionic gelation method. The microcapsules were evaluated for surface morphology and particle shape by scanning electron microscope. Microcapsules were also evaluated for their microencapsulation efficiency, in vitro wash-off mucoadhesion test, in vitro drug release and in vivo study...
2008: AAPS PharmSciTech
Barbara Luppi, Federica Bigucci, Teresa Cerchiara, Roberto Mandrioli, Anna Maria Di Pietra, Vittorio Zecchi
Nano and micro preparative technologies for the realization of pharmaceutical carriers represent an actual strategy for reaching the therapeutic success of drugs, particularly in the case of peptidic drugs. Vancomycin is here entrapped in carriers composed by a swellable, mucoadhesive and biodegradable albumin core, coated with fatty acids able to improve a colon-specific release. Bovine serum albumin nanospheres (core) were prepared from protein solutions using a coacervation method followed by thermal cross-linking at different temperature, or from protein solutions at different pHs using a coacervation method followed by thermal cross-linking at 75 degrees C...
June 24, 2008: International Journal of Pharmaceutics
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