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The release of drugs from solid drug delivery materials has been studied intently in recent years. Quantitative analyses achieved from in vitro dissolution becomes easier if a zero-order mathematical model is used. Non-gelatin nutraceutical hard-shell capsules of zero size (approximately 0.7-0.8 cm) were produced from carrageenan-based natural poly...
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... The pH of the PBI dispersion was then set to 8.90 ± 0.05 using NaOH (1.0 or 0.1 mol L −1 ), and the dispersion that was subsequently obtained was heated at 115-117°C for 20 min. 37,44,45 Aqueous ethanolic (50%) curcumin (Cu) solution was incorporated into aggregated PBI dispersion (PBA) to adjust the final concentration of curcumin to 1.4 mg mL −1 (curcumin to protein ratio of 1:50 w/w). The final ethanol concentration within the PBA solution was less than 2.0 mL L −1 . ...
BACKGROUND
Protein gels are used for different purposes, such as providing good texture, serving as fat replacers, and enhancing the nutritional and functional characteristics of foods. They can also deliver controlled release agents for sensitive drugs. The objective of this study was to investigate the impact of κ‐carrageenan (kcr) concentration (0, 1.5, 3, and 4.5 mg g⁻¹) on the morphological and physicochemical properties and release behavior of glucono‐δ‐lactone (GDL)‐induced pinto bean protein aggregate (PBA) gels.
RESULTS
When κ‐carrageenan concentration increased from 0 to 1.5 and 3 mg.g⁻¹, the firmness of the samples increased significantly, by 2.04 and 3.7 fold, respectively (P < 0.05). A compact and homogenous network with considerable strength and maximum water‐holding capacity (97.52 ± 1.17%) was obtained with the addition of 3 mg g⁻¹ κ‐carrageenan to the gel system. Further increasing the κ‐carrageenan concentration to 4.5 mg g⁻¹ produced a coarse gel structure with higher storage modulus (G′), firmness (6.30‐fold), thermal stability, and entrapment efficiency (85.6%). Depending on the κ‐carrageenan concentration, various microstructures from protein continuous phase to κ‐carrageenan continuous phase were observed. The release test indicated that 70.25% of the loaded curcumin was released in the simulated gastrointestinal tract for pure PBA gels. In contrast, for binary gels containing 4.5 mg g⁻¹ κ‐carrageenan, curcumin was protected in the upper gastrointestinal tract, and 64.45% of loaded curcumin was delivered to the colon.
CONCLUSION
Our study showed that κ‐carrageenan/PBA gels had high entrapment efficiency and could protect curcumin in the upper gastrointestinal tract. The hydrogels are therefore very valuable for colon‐targeting delivery purposes. © 2022 Society of Chemical Industry.
... In that Q t = drug release over time t; Q 0 = amount of drug at zero time; K 0 = zero order constant; K 1 = first order rate constant; K H t (Higuchi constant); M t & M ∞ = amount of drug release at time t and infinitive time; M 0 = amount drug at zero time; M t = amount of drug remaining at time t; k = Korsmeyer-Peppas an dHixon-Crowell constant; n = diffusion exponent for releases mechanism; n = 0.45 indicated Case1 or fickian diffusion; 0.45 < n < 0.89 = anomalous behavior or non-fickian diffusion; n = 0.89 (Case 11 transport) and n > 0.89 = super case II transport (Pudjiastuti et al., 2020). ...
Quercetin (QT) is a flavonoid that exhibits anti-oxidant and chemo-preventive activity. This research work aimed to develop surface-modified bilosomes (BS) of QT. The BS was prepared by the solvent evaporation method and optimized by the Box-Behnken design. The optimized QT-BS (QT-BS3opt) displayed vesicle size (143.51 nm), PDI (0.256), zeta potential (−15.4 mV), and entrapment efficiency (89.52%). Further, the optimized QT-BS formulation was coated with chitosan (CS). The XRD diffractogram of CS-QT-BS3opt1 did not exhibit extensive peaks of QT, revealing that QT is properly encapsulated in the polymer matrix. The QT-BS3opt and CS-QT-BS3opt1 exhibited sustained-release (86.62 ± 3.23% and 69.32 ± 2.57%, respectively) up to 24 h with the Korsmeyer-Peppas kinetic model (R2 =0.9089). CS-QT-BS3opt1 exhibited significantly (P < .05) high flux, i.e. 4.20-fold more than pure QT dispersion and 1.27-fold higher than QT-BS3opt. CS-QT-BS3opt1 showed significantly greater bio-adhesion (76.43 ± 2.42%) than QT-BS3opt (20.82 ± 1.45%). The antioxidant activity showed that QT from CS-QT-BS3opt1 has more remarkable (P < .05) antioxidant activity at each concentration than pure QT. The CS-QT-BS3opt1 exhibited 1.61-fold higher cytotoxicity against MFC7 and 1.44-fold higher cytotoxicity against MDA-MB-231 than pure QT. The CS-QT-BS3opt1 displayed a significantly greater antimicrobial potential against E. coli than against S. aureus. From all these findings, it could be concluded that surface-modified QT-BS might be an effective approach for increasing the efficacy of QT in the treatment of certain ailments.
... In vitro release data require different equations and kinetic models to explain the kinetics of the release [41]. Release kinetics are important in understanding the absorption, distribution, metabolism, and excretion of the active substance after ingestion [42]. Some mathematical operations and equations are needed to explain the mechanism of drug release from beads. ...
Today, treating diseases requires increasing the patient's living standard rather than just applying a
classical treatment protocol. In this study, it was aimed at facilitating drug intake, reduce the dose of the active
substance, reduce the number of daily doses to be taken, reduce or eliminate possible side and/or toxic effects, transport
the active substance to the target area and make as much bioavailability from the active substance as possible too. For
this purpose, in our study, hydrogel bead formulations with ionotropic gelation technique were developed using
ampicillin sodium as a model drug and sodium alginate and HPMC K100 as polymer. CaCl2 was used as a crosslinking
agent. While developing a new drug delivery system formulation, size, morphology with SEM, in vitro release profiles,
release kinetics, encapsulation efficiencies, drug loading capacities, yields, and swelling capacities, FT-IR and XRD
analysis were evaluated in the hydrogel beads depending on the amount of the polymer and crosslinking agent. It has
been made possible to extend the duration of drug action by changing the amount of polymer and crosslinker ratios in
oral drug delivery of ampicillin sodium with alginate beads. Thus, it is likely to increase patient compliance as well as
to reduce drug-related side and/or toxic effects with less dosing.
KEYWORDS: Ampicillin sodium; beads; drug delivery system; HPMC; sodium alginate.
... The alternative materials developed for hard capsules include alginate [8], carrageenan [9], hypromellose (HPMC) [6] and strong cellulosic fibre from different plant materials such as Dracanea reflexa [10] and Tridax procumbens [11]. However, there are still some disadvantages that must be improved for future use, such as the need for alginate hard capsules to be crosslinked with another agent to form a rigid gel [8]. ...
... However, we found that carrageenan has good potential for development as an oligomer-based drug-delivery system as it is easily hydrolysed by a weak acid, such as citrate buffer [13]. Accordingly, the oligomerisation of carrageenan should be performed at a controlled temperature and time, i.e., at 70 °C for 5 h [9], to form a homogeneous solution and control the oligomers formed. One purpose of this oligomerisation process is to control the rate of disintegration of carrageenan-based hard capsules. ...
... However, we found that carrageenan has good potential for development as an oligomer-based drug-delivery system as it is easily hydrolysed by a weak acid, such as citrate buffer [13]. Accordingly, the oligomerisation of carrageenan should be performed at a controlled temperature and time, i.e., at 70 • C for 5 h [9], to form a homogeneous solution and control the oligomers formed. One purpose of this oligomerisation process is to control the rate of disintegration of carrageenan-based hard capsules. ...
Intense efforts to develop alternative materials for gelatine as a drug-delivery system are progressing at a high rate. Some of the materials developed are hard capsules made from alginate, carrageenan, hypromellose and cellulose. However, there are still some disadvantages that must be minimised or eliminated for future use in drug-delivery systems. This review attempts to review the preparation and potential of seaweed-based, specifically carrageenan, hard capsules, summarise their properties and highlight their potential as an optional main component of hard capsules in a drug-delivery system. The characterisation methods reviewed were dimensional analysis, water and ash content, microbial activity, viscosity analysis, mechanical analysis, scanning electron microscopy, swelling degree analysis, gel permeation chromatography, Fourier-transform infrared spectroscopy and thermal analysis. The release kinetics of the capsule is highlighted as well. This review is expected to provide insights for new researchers developing innovative products from carrageenan-based hard capsules, which will support the development goals of the industry.
... These results further confirm that the outcomes of KET and LYS crystallization are two different structural entities and demonstrate that the two forms are characterized by different IDRs. In vitro dissolution is an important factor in defining drug absorption, distribution, metabolism, and excretion (ADME), and different IDRs among drugs can allow for the development of formulations with different release kinetic profiles [29]. Commercial KLS (representative of KET-LYS P1) has been reported to exhibit fast in vivo absorption and onset of action [22]; thus, the faster dissolution observed for KET-LYS P2 compared to KET-LYS P1 may suggest that the newly synthesized salt form (KET-LYS P2) could be characterized by a faster absorption compared to the commercialized KLS. ...
Ketoprofen–l-lysine salt (KLS) is a widely used nonsteroidal anti-inflammatory drug. Here, we studied deeply the solid-state characteristics of KLS to possibly identify new polymorphic drugs. Conducting a polymorph screening study and combining conventional techniques with solid-state nuclear magnetic resonance, we identified, for the first time, a salt/cocrystal polymorphism of the ketoprofen (KET)–lysine (LYS) system, with the cocrystal, KET–LYS polymorph 1 (P1), being representative of commercial KLS, and the salt, KET–LYS polymorph 2 (P2), being a new polymorphic form of KLS. Interestingly, in vivo pharmacokinetics showed that the salt polymorph has significantly higher absorption and, thus, different pharmacokinetics compared to commercial KLS (cocrystal), laying the basis for the development of faster-release/acting KLS formulations. Moreover, intrinsic dissolution rate (IDR) and electronic tongue analyses showed that the salt has a higher IDR, a more bitter taste, and a different sensorial kinetics compared to the cocrystal, suggesting that different coating/flavoring processes should be envisioned for the new compound. Thus, the new KLS polymorphic form with its different physicochemical and pharmacokinetic characteristics can open the way to the development of a new KET–LYS polymorph drug that can emphasize the properties of commercial KLS for the treatment of acute inflammatory and painful conditions.
... M t and M 1 are cumulative drug release at time t and infinite time, respectively; k is rate constant of NS particle's structural and geometric characteristics feature, t is the release time and n denotes diffusional exponent indicating release mechanism. When n = 0.45 (Case I or Fickian diffusion), 0.45 < n < 0.89 (anomalous behavior or non-Fickian transport), n = 0.89 (Case II transport) and n > 0.89 (Super Case II), based on the exponent value release mechanisms were reported (Pudjiastuti et al., 2020). ...
In the current study, four formulae (BNS1-BNS4) of butenafine (BTF) loaded nanosponges (NS) were fabricated by solvent emulsification technology, using different concentration of ethyl cellulose (EC) and polyvinyl alcohol (PVA) as a rate retarding polymer and surfactant, respectively. Prepared NS were characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE) and drug loading (DL). Nanocarrier BNS3 was optimized based on the particle characterizations and drug encapsulation. It was further evaluated for physicochemical characterizations; FTIR, DSC, XRD and SEM. Selected NS BNS3 composed of BTF (100 mg), EC (200 mg) and 0.3% of PVA showed, PS (543 ± 0.67 nm), PDI (0.330 ± 0.02), ZP (-33.8 ± 0.89 mV), %EE (71.3 ± 0.34%) and %DL (22.8 ± 0.67%), respectively. Fabricated NS also revealed; polymer-drug compatibility, drug-encapsulation, non-crystalline state of the drug in the spherical NS as per the physicochemical evaluations. Optimized NS (BNS3) with equivalent amount of (1%, w/w or w/v) BTF was incorporated into the (1%, w/w or w/v) carbopol gel. BTF loaded NS based gel was then evaluated for viscosity, spreadability, flux, drug diffusion, antifungal, stability and skin irritation studies. BNS3 based topical gels exhibited a flux rate of 0.18 (mg/cm2.h), drug diffusion of 89.90 ± 0.87 % in 24 h with Higuchi model following anomalous non-Fickian drug release. The BNS3 based-gel could be effective against pathogenic fungal strains.
... After suitable dilutions, drug release was calculated from absorbance determined by UV spectrophotometric analysis. Different kinetic models were applied to study release kinetics and data analysis was done using (DD solver, 1.0 (Trial version), Nanjing, China) (Pudjiastuti et al., 2020). ...
Valganciclovir HCl (VGH) is the widely used drug for the treatment of Cytomegalovirus (CMV) retinitis infection with an induction dose of 900mg twice a day and a maintenance dose of 900mg. This required dose of the drug also leads to multiple side effects due to repeated administration. The research was highlighted to develop, formulate, optimize and evaluate Single-Core Osmotic Pump (SCOP) tablet of VGH with the dose of 450mg to reduce dosing frequency and associated side effects. . The decrease in dose also minimize the hepatic and nephrotic load. The optimized batch of formulation was subjected to comparative in vitro and in vivo evaluation. The tablet core composition is the primary influencer of the drug delivery fraction in a zero-order, whereas the membrane characteristics control the drug release rate. In-vivo pharmacokinetic studies revealed that the newly developed osmotic formulation has controlled zero-order release for 24 hours with a single dose of 450mg while the marketed formulation requires twice administration within 24 hours to maintain the plasma concentration in the therapeutic window. The developed formulation can be the promising option for the treatment of CMV retinitis with the minimum dose and dosing frequency.
Drug delivery carrier is a mechanism used to distribute drugs into the body. Drug delivery carrier which is widely used in drug delivery are capsules. Carrageenan-alginate is a vegetable polymer that is expected to be a substitute for gelatin in making capsules. The purpose of this research is to prepare,and characterize carrageenan-alginate hard-shell capsules with polyethylene glycol plasticizers as drug delivery carrier materials. Hard-shell capsules were made from carrageenan-alginate and PEG copolymers with variations in the volume of 0.5 ml (CAP1), 1.0 ml (CAP2), 1.5 ml (CAP3), and 2.0 ml (CAP4). Hard-shell capsules characterization includes swelling, tensile, dissolution, disintegration, kinetic, Fourier-transform Infrared Spectroscopy (FTIR), and Scanning Electron Microscope (SEM) tests. The hard-shell capsules with the most optimum mechanical properties were CAP3 capsules with % swelling of 413.2%, stress values of 101.4 Mpa, strain values of 0.27, and young modulus of 1297.9 Mpa. Dissolution results showed that the salicylamide drug was distributed 11% in buffer phosphate at the 120th minute. Disintegration results for 37 minutes. FTIR results show there are hydrogen bonds between carrageenan, alginate, and PEG. SEM results showed the hard-shell capsules had a smooth and porous surface morphology and cross-section, which was an average of 4.949 µm. The most linear release kinetic test results using the Higuchi model at pH 6.8 with reaction rate constants of 1.002 M.s−1/2 and R² = 0.967, so that the Carrageenan-alginate copolymer hard-shell capsules with PEG plasticizers can be used as controlled release drug delivery carriers.
Valganciclovir HCl (VGH) is the widely used drug for the treatment of cytomegalovirus (CMV) retinitis infection with an
induction dose of 900 mg per oral (p.o.) twice a day and a maintenance dose of 900 mg (p.o.). This required dose of the
drug also leads to multiple side effects due to repeated administration. The research was highlighted to develop, formulate,
optimize, and evaluate single-core osmotic pump (SCOP) tablet of VGH with the dose of 450 mg to reduce dosing frequency
and associated side effects. The decrease in dose also minimizes the hepatic and nephrotic load. The optimized batch of
the formulation was subjected to comparative in vitro and in vivo evaluation. The tablet core composition is the primary
influencer of the drug delivery fraction in a zero order, whereas the membrane characteristics control the drug release rate.
In vivo pharmacokinetic studies revealed that the newly developed osmotic formulation has controlled zero-order release
for 24 h with a single dose of 450 mg while the marketed formulation requires twice administration within 24 h to maintain
the plasma concentration in the therapeutic window. The pharmacokinetic study demonstrated that the developed formula�tion has the area under curve (AUC) of 58.415 µg h/ml with single dose while the marketed formulation shows the AUC of
about 37.903 µg h/ml and 31.983 µg h/ml for first and second dose, respectively. The large AUC demonstrates the extended
release of drug with a single dose and effective plasma concentration. Hence, the developed formulation can be a promising
option for the treatment of CMV retinitis with the minimum dose and dosing frequency.
______________________________________________________________________________________________________ The purpose of present exploration was to modify kappa (k)-Carrageenan, by crosslinking, and assessed it as a tablet disintegrant to strengthen the solubility of the drug (aceclofenac) in tablet formulation. Modified k-Carrageenan was synthesized by reacting it with epichlorhydrin at heterogenous conditions. The swelling action of the product was investigated in order to optimize reaction circumstances for chemical cross-linking. Best modified k-Carrageenan procured by optimizing the reaction conditions and it was characterized for swelling index, particle size distribution, solubility, viscosity, gel strength and Fourier transform infrared spectroscopy (FTIR). Influence of modified k-Carrageenan on dissolution profile of therapeutic was also investigated along with other evaluation parameters. Modified k-Carrageenan exhibiting significant swelling index which is comparable to that of superdisintegrants. On comparative investigation as a tablet disintegrant by preparing anhydrous dicalcium phosphate tablet, modified k-Carrageenan showed disintegration time less than 20 seconds. Dissolution of aceclofenac (Class II) tablet formulaion utilizing modified k-Carrageenan was comparable with commercially available superdisintegrants. Faster dissolution of the accommodated drug was achieved with modified k-Carrageenan which was comparable with dissolution of the tablet formulation containing other superdisintegrants. The competent concentration of k-Carrageenan was found to be 5-15% as tablet disintegrant. Modified k-Carrageenan might be encouraging tablet disintegrant in fast dissolving formulations and can be worn in direct compression method.
