Development of resistant corn starch for use as an oral colon-specific nanoparticulate drug carrier

2018 ◽  
Vol 90 (6) ◽  
pp. 1073-1084 ◽  
Author(s):  
Norul Nazilah Ab’lah ◽  
Nagarjun Konduru Venkata ◽  
Tin Wui Wong
Keyword(s):  
Molecular Weight ◽  
Drug Release ◽  
Resistant Starch ◽  
Corn Starch ◽  
Drug Carrier ◽  
Scanning Calorimetry ◽  
Native Starch ◽  
Heat Moisture Treatment ◽  
Moisture Treatment

Abstract Starch is constituted of amylose and amylopectin. Debranching of amylopectin converts it into amylose thereby producing resistant starch which is known to be less digestible by the amylase. This study designed resistant starch using acid hydrolysis and heat-moisture treatment methods with native corn starch as the starting material. Both native and processed starches were subjected to Fourier transform infrared spectroscopy, X-ray diffractometry, differential scanning calorimetry and molecular weight analysis. They were nanospray-dried into nanoparticles with 5-fluorouracil as the drug of interest for colon cancer treatment. These nanoparticles were subjected to size, zeta potential, morphology, drug content and in vitro drug release analysis. Heat-moisture treatment of native corn starch enabled the formation of resistant starch through amylopectin debranching and molecular weight reduction thereby enhancing hydrogen bonding between the starch molecules at the amorphous phase and gelatinization capacity. The nanoparticles prepared from resistant starch demonstrated similar drug release as those of native starch in spite of the resistant starch had a lower molecular weight. The resistant starch is envisaged to be resistant to the digestive action of amylase in intestinal tract without the formed nanoparticles exhibiting excessively fast drug release in comparison to native starch. With reduced branching, it represents an ideal precursor for targeting ligand conjugation in design of oral colon-specific nanoparticulate drug carrier.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Heat-Moisture Treatment Further Reduces In Vitro Digestibility and Enhances Resistant Starch Content of a High-Resistant Starch and Low-Glutelin Rice

Foods ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 2562
Author(s):  
Zhiyuan Li ◽  
Dongshu Guo ◽  
Xiao Li ◽  
Zhaocheng Tang ◽  
Xitie Ling ◽  
...  
Keyword(s):  
Resistant Starch ◽  
Kidney Diseases ◽  
Starch Content ◽  
Rice Flour ◽  
Targeted Mutagenesis ◽  
In Vitro Digestibility ◽  
Food Ingredient ◽  
Heat Moisture Treatment ◽  
Moisture Treatment

A novel rice germplasm sbeIIb/Lgc1 producing grains rich in resistant starch (RS) but low in glutelin has been developed through CRISPR/Cas9-mediated targeted mutagenesis for its potential benefits to patients with diabetes and kidney diseases. In this study, a hydrothermal approach known as heat-moisture treatment (HMT) was identified as a simple and effective method in reinforcing the nutritional benefits of sbeIIb/Lgc1 rice. As a result of HMT treatment at 120 °C for 2 h, significant reductions in in vitro digestibility and enhancements in RS content were observed in sbeIIb/Lgc1 rice flour when the rice flour mass fraction was 80% and 90%. The low-glutelin feature of sbeIIb/Lgc1 rice was not compromised by HMT. The potential impacts of HMT on a range of physicochemical properties of sbeIIb/Lgc1 rice flour have also been analyzed. HMT resulted in a darker color of rice flour, alteration in the semi-crystalline structure, an increase in gelatinization temperatures, and reductions in the pasting viscosities as the moisture content increased. This study provides vital data for the food industry to facilitate the application of this dual-functional rice flour as a health food ingredient.

Facile Synthesis of Chitosan Based-(AMPS-co-AA) Semi-IPNs as a Potential Drug Carrier: Enzymatic Degradation, Cytotoxicity, and Preliminary Safety Evaluation

2019 ◽  
Vol 16 (3) ◽  
pp. 242-253 ◽  
Author(s):  
Kaleem Ullah ◽  
Muhammad Sohail ◽  
Abdul Mannan ◽  
Haroon Rashid ◽  
Aamna Shah ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Cytotoxicity ◽  
Oral Drug ◽  
Specific Enzyme ◽  
Oral Toxicity ◽  
Scanning Calorimetry

Objective: The study describes the development of chitosan-based (AMPS-co-AA) semi-IPN hydrogels using free radical polymerization technique. Methods: The resulting hydrogels were characterized using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), X-Ray diffraction (XRD), and Scanning Electron Microscopy (SEM). The successful crosslinking of chitosan, 2- Acrylamido-2-Methylpropane Sulfonic Acid (AMPS), and Acrylic Acid (AA) was confirmed by FT IR. Unloaded and drug-loaded hydrogels exhibited higher thermal stability after crosslinking compared to the individual components. XRD confirmed the decrease in crystallinity after hydrogel formation and molecular dispersion of Oxaliplatin (OXP) in the polymeric network. SEM showed rough, vague and nebulous surface resulting from crosslinking and loading of OXP. Results: The experimental results revealed that swelling and drug release were influenced by the pH of the medium being low at acidic pH and higher at basic pH. Increasing the concentration of chitosan and AA enhanced the swelling, drug loading and drug release while AMPS was found to act inversely. Conclusion: It was confirmed that the hydrogels were degraded more by specific enzyme lysozyme as compared to the non-specific enzyme collagenase. In-vitro cytotoxicity suggested that the unloaded hydrogels were non-cytotoxic while crude drug and drug-loaded hydrogel exhibited dose-dependent cytotoxicity against HCT-116 and MCF-7. Results of acute oral toxicity on rabbits demonstrated that the hydrogels are non-toxic up to 3900 mg/kg after oral administration, as no toxicity or histopathological changes were observed in comparison to control rabbits. These pH-sensitive hydrogels appear to provide an ideal basis as a safe carrier for oral drug delivery.

Preparation of poly(sebacic anhydride) and polylactic acid pills used as drug carrier for levofloxacin controlled release

2013 ◽  
Vol 33 (7) ◽  
pp. 659-664 ◽  
Author(s):  
Zhuan Zhang ◽  
Liao-Bing Chen ◽  
Jie Gao ◽  
Feng Bao ◽  
Jing Yin ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Controlled Release ◽  
Drug Release ◽  
Polylactic Acid ◽  
Release Rate ◽  
Drug Carrier ◽  
Antibacterial Drug ◽  
Molecular Weights ◽  
Zero Order Release

Abstract A biodegradable local drug release system consisting of poly(sebacic anhydride) and polylactic acid was developed for the purpose of osteomyelitis therapy. Five kinds of poly(sebacic anhydride) with different molecular weights were synthesized, and levofloxacin was chosen as a model antibacterial drug in the in vitro release within 38 days. As the molecular weight of poly(sebacic anhydride) increased, the melting point (Tm) of the matrices increased and the surface morphology became smoother. Consequently, the initial burst effect was reduced and the release rate significantly decreased. In addition, the kinetics of pills containing poly(sebacic anhydride) (Mw=13,000) were close to zero order release. The release profile reveals that the thermodynamic properties and morphology of these matrices, which are affected by the molecular weight, are essential for developing controllable delivery systems. The drug release rate could be easily controlled by the molecular weight of the poly(sebacic anhydride). Finally, these prospective results allow the biodegradable controlled release systems to be employed as carriers for the treatment of chronic osteomyelitis, as well as for other medical applications.

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals Physicochemical and Antifungal Properties of Clotrimazole in Combination with High-Molecular Weight Chitosan as a Multifunctional Excipient

Marine Drugs ◽  
2020 ◽  
Vol 18 (12) ◽  
pp. 591
Author(s):  
Bożena Grimling ◽  
Bożena Karolewicz ◽  
Urszula Nawrot ◽  
Katarzyna Włodarczyk ◽  
Agata Górniak
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Weight Ratio ◽  
Scanning Calorimetry ◽  
Minimal Inhibitory Concentrations ◽  
Dissolution Tests ◽  
Effective Combination ◽  
The Impact ◽  
High Molecular Weight Chitosan

Chitosans represent a group of multifunctional drug excipients. Here, we aimed to estimate the impact of high-molecular weight chitosan on the physicochemical properties of clotrimazole–chitosan solid mixtures (CL–CH), prepared by grinding and kneading methods. We characterised these formulas by infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffractometry, and performed in vitro clotrimazole dissolution tests. Additionally, we examined the antifungal activity of clotrimazole–chitosan mixtures against clinical Candida isolates under neutral and acid conditions. The synergistic effect of clotrimazole and chitosan S combinations was observed in tests carried out at pH 4 on Candida glabrata strains. The inhibition of C. glabrata growth reached at least 90%, regardless of the drug/excipient weight ratio, and even at half of the minimal inhibitory concentrations of clotrimazole. Our results demonstrate that clotrimazole and high-molecular weight chitosan could be an effective combination in a topical antifungal formulation, as chitosan acts synergistically with clotrimazole against non-albicans candida strains.

scholarly journals Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
Author(s):  
Anuj Chawla ◽  
Pooja Sharma ◽  
Pravin Pawar
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Naproxen Sodium ◽  
Drug Loading ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
S 100 ◽  
Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

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