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The comparison of the kinetic parameters release of RH from the different matrices based on zero order, first order, Higuchi model, and Krosmayer-Peppas model plots.
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Alginate (Alg) is a polyanionic polymer whereas chitosan (Ch) is a polycationic polymer. The purpose of this study was to compare the swelling, mucoadhesive, and release of ranitidine HCl (RH) from the spherical matrices of Alg, Ch, Alg-Ch and calcium alginate-chitosan (Ca Alg-Ch). The spherical matrices containing RH were prepared by incorporating...
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Alginate (Alg) is a polyanionic polymer whereas chitosan (Ch) is a polycationic polymer. The purpose of this study was to compare the swelling, mucoadhesive, and release of ranitidine HCl (RH) from the spherical matrices of Alg, Ch, Alg-Ch and calcium alginate-chitosan (Ca Alg-Ch). The spherical matrices containing RH were prepared by incorporating...
Citations
... The cross-linking process occurs when the negatively charged member of the tripolyphosphate polyanion interacts with the positively charged amine group in a complex manner [16]. were irregularly shaped and the surface of the chitosan-alginate and chitosan-alginate-calcium is smoother than the surface chitosan matrix [17]. Thus, it can be concluded that the use of chitosan as a microparticle matrix tends to produce non-spherical microparticle shapes and uneven surfaces since during the drying process the water adsorbed on the wet microparticles and pushed out. ...
Objective: The objective of this research is to investigate the effect of Hydroxypropyl Methylcellulose (HPMC) concentration as a gel base for chitosan microparticle-containing beetroot (Beta vulgaris, Linn) toward gels stability and skin brightening effect. Methods: Ionic gelation was used to make microparticle using chitosan 1% solution and beetroot dry extract as active component. Scanning Electron Microscope (SEM) and active substance loading were used for physical characterisation. The MP then was added to HPMC-based gels at 0.5, 1.0, and 1.5% w/w. Gels were tested for viscosity, pH, and active component stability. Gels were tested for skin lightening on humans. Results: Results reveal beetroot extract may be loaded into chitosan microparticle with a Drug Loading (DL) of 23.27±0.057% w/w. HPMC gels had a pH of 5-5.4 and increased viscosity related with HPMC content. Gels showed colour instability after 6 cooling-heating cycles and decreased betanin levels on day 7 at 40±2 °C and RH 75±5%. HPMC 0.5% gel brightened human skin more than other HPMC gels. Conclusion: The 0.5% HPMC gel base had the smallest betanin reduction during the accelerated stability test, compared to the 1.0 and 1.5% HPMC gels. The formulation of chitosan microparticle gel loading beetroot extract with 0.5% HPMC gel base had brightened skin better than the other two formulae.
... Another endothermic peak is prominent in the samples of the physical mix, and SFT HCQ starts before 50° and extends to around 100° (Fig. 1 b2). This can be attributed to the loss of water from hydrophilic polymers [100]. The endothermic melting peak was absent in the DSC thermogram of SFT HCQ, suggesting the possibility of the drug dissolving inside the hydrophilic carrier and conversion to an amorphous form as supported by PXRD results [35,98]. ...
Hydroxychloroquine (HCQ) was repurposed for COVID-19 treatment. Subtherapeutic HCQ lung levels and cardiac toxicity of oral HCQ were overcome by intratracheal (IT) administration of lower HCQ doses. The crosslinker-free supercritical fluid technology (SFT) produces aerogels and impregnates them with drugs in their amorphous form with efficient controlled release. Mechanistic physiologically based pharmacokinetic (PBPK) modeling can predict the lung’s epithelial lining fluid (ELF) drug levels. This study aimed to develop a novel HCQ SFT formulation for IT administration to achieve maximal ELF levels and minimal cardiac toxicity. HCQ SFT formulation was prepared and evaluated for physicochemical, in vitro release, pharmacokinetics, and cardiac toxicity. Finally, the rat HCQ ELF concentrations were predicted using PBPK modeling. HCQ was amorphous after loading into the chitosan-alginate nanoporous microparticles (22.7±7.6 μm). The formulation showed a zero-order release, with only 40% released over 30 min compared to 94% for raw HCQ. The formulation had a tapped density of 0.28 g/cm3 and a loading efficiency of 35.3±1.3%. The IT administration of SFT HCQ at 1 mg/kg resulted in 23.7-fold higher bioavailability, fourfold longer MRT, and eightfold faster absorption but lower CK-MB and LDH levels than oral raw HCQ at 4 mg/kg. The PBPK model predicted 6 h of therapeutic ELF levels for IT SFT HCQ and a 100-fold higher ELF-to-heart concentration ratio than oral HCQ. Our findings support the feasibility of lung-targeted and more effective SFT HCQ IT administration for COVID-19 compared to oral HCQ with less cardiac toxicity.
Graphical abstract
... This model is also based on Fick's diffusion law and was developed to describe the release from different porous matrices, especially for the release of poorly soluble drugs encapsulated in semi-solid or solid matrices. Moreover, according to this model, the release of active ingredients is increased with decreasing tortuosity [113]. It is possible that due to the concentrations of GEL and SA used in the encapsulation process, strong ionic interactions of the polymers occur, resulting in increased tortuosity of the hydrogels. ...
Grape pomace is a byproduct of wineries and a rich source of phenolic compounds that can exert multiple pharmacological effects when consumed and enter the intestine where they can then be absorbed. Phenolic compounds are susceptible to degradation and interaction with other food constituents during digestion, and encapsulation may be a useful technique for protecting phenolic bioactivity and controlling its release. Therefore, the behavior of phenolic-rich grape pomace extracts encapsulated by the ionic gelation method, using a natural coating (sodium alginate, gum arabic, gelatin, and chitosan), was observed during simulated digestion in vitro. The best encapsulation efficiency (69.27%) was obtained with alginate hydrogels. The physicochemical properties of the microbeads were influenced by the coatings used. Scanning electron microscopy showed that drying had the least effect on the surface area of the chitosan-coated microbeads. A structural analysis showed that the structure of the extract changed from crystalline to amorphous after encapsulation. The phenolic compounds were released from the microbeads by Fickian diffusion, which is best described by the Korsmeyer–Peppas model among the four models tested. The obtained results can be used as a predictive tool for the preparation of microbeads containing natural bioactive compounds that could be useful for the development of food supplements.
... Aliquot was transferred to 20 mL volumetric flask and adjusted the volume till the mark by using simulated gastric fluid pH 1.2 (withouth enzyme). [13] The absorbances were measured with spectrophotometer UV (Shimadzu UV-1800) under the maximum wavelength at 277 nm. The measurement result of metronidazole microcapsule preparation meet the requirements of microcapsule particle size, which is not more than 5 mm [14] 3 ...
The oral conventional metronidazole dosage forms have a short duration of action due to gastric emptying process, hence the treatment of ulcus pepticum using metronidazole become less effective. Due to retaining the dosage form in the stomach, a preparation form of sustained released drug delivery systems has been developed. The aim of this study was to developed a sustained released drug delivery systems of metronidazole using alginate and chitosan as polymers that could last longer in stomach. The formulation consisted of variatons in chitosan 0.5%, 0.75% and 1%. The drug released test was carried out using paddle method in simulated gastric medium pH 1.2 at 37°C. The dissolution test results showed that formula with 0.75% of chitosan giving the best sustained released effect and the kinetics drug realeased of microcapsule followed Higuchi order. Based on the results of the study, it can be concluded that microcapsules of metronidazole with a combination of alginate and chitosan can be prepared as sustained released formulation.
... Menurut Ton et al., (2016), bahan penyalut merupakan salah satu faktor yang mempengaruhi efisiensi enkapsulasi. Penggabungan kitosan dan STPP menyebabkan terjadi interaksi sambung silang polimer sehingga meningkatkan nilai tortuositas (Arianto et al., 2015). Tortuositas adalah besaran yang terkait dengan jalur yang dilewati oleh fluida dalam suatu medium berpori (Batys and Weroński, 2014). ...
... They possess unique physicochemical characteristics because of their reduced sizes and enhanced surface areas. CNp also finds applications in drug delivery and macromolecules whereby the active ingredients in the composition can be delivered to targeted sites (Perera and Rajapakse, 2013;Arianto et al., 2015). Furthermore, it is also useful as a carrier of antioxidants, antimicrobial agents, enzymes, minerals, and probiotics (Ojagh et al., 2010;Rajalakshmi et al., 2013). ...
Chitosan nanoparticles (CNp), nickel-chitosan nanoparticles (Ni-CNp), and copper-chitosan nanoparticles (Cu-CNp) were synthesized from pure chitosan. The samples were characterized using Energy-Dispersive X-ray Spectroscopy (EDS), Transmission Electron Microscopy (TEM), Fourier-Transform Infra-Red (FTIR), and X-ray Diffraction (XRD). Their inhibitory and bactericidal potentialities were tested against Salmonella sp. and Shigella sp. at 1000, 500, 250, and 125 mg mL⁻¹. The EDS results revealed the elemental composition of the samples. At 1000 mg mL⁻¹: against Salmonella sp., MIC values for CNp, Ni-CNp, and Cu-CNP were 20.4 ± 0.64, 25.6 ± 0.71, and 34.3 ± 0.57 mgmL⁻¹, respectively; for Shigella sp., the MIC values for CNp, Ni-CNp, and Cu-CNP were 20.8 ± 0.64, 24.2 ± 0.21, and 23.57 ± 0.58 mgmL⁻¹, respectively. This trend was also observed at 500, 250, and 125 mg mL⁻¹. The results established that the incorporation of heavy metals into CNp induced more antimicrobial potency against Salmonella sp. and Shigella sp.
... For alginate emulsions with the selected extract and essential oil were prepared with a solution of sodium alginate (DAHIPRO, 1.5 % w/v) and CaCl 2 (DAHIPRO, 1.3 % w/v) by dilution in distilled water at 35°C. Each dilution was left to stir at 200 rpm on a magnetic stirrer for 2 hours (19,20). Different emulsions were prepared by mixing clove essential oil or extract with metronidazole and alginate. ...
Objectives:The alginate microspheres were prepared
with methanol extract of rue and essential oil of
clove with metronidazole evaluating their biological
and physicochemical activities. Materials and
methods: Microspheres were evaluated with their
sphericity, encapsulation efficiency, degradation,
and release kinetics with mathematical models.
Also, their hemocompatibility and antiamebic
activity were studied on hemolytic, proteolytic, and
erythrophagocytic activities of Entamoeba histolytica.
Results: Microspheres were obtained with sphericity
equal to one, with encapsulation efficiency greater
than 50 % (except CEO in 220 nm). Their degradation
was recorded between 8 %-12 % in acidic and
basic pH. In addition, its release kinetics had a
burst constant in almost all the treatments, with the
behavior of Korsmeyer-Peppas and Peppas-Sahlin
being of pseudofickian behavior. The microspheres
were hemocompatible according to the regulations
(<10 %) and additionally decreased virulence
factors of the amoeba such as hemolytic, proteolytic,
erythrophagocytic activities. Conclusions: The
microspheres obtained could be a possible treatment
against E. histolytica. Still, other toxicity
parameters have to be determined (i.e., cytotoxicity,
cytocompatibility, biosafety, body weight, survival
rate, weight index of main organs, histopathology
of main organs, serum biochemical, etc.), as well
as physicochemical parameters such as differential
scanning calorimetry, Fourier-transform infrared
spectroscopy and viscosity.
... Penelitian terkini melaporkan, beberapa cara untuk meningkatkan kemampuan biopolimer alginat sebagai enkapsulan yakni dengan mengkompositkan dengan polimer lain seperti menggunakan kombinasi alginatmontmorillonite (Kevadiya et al., 2010), komposit alginat-kitosan dengan CaCl2 (Arianto et al., 2014), dan polietilen glikol (PEG) (Wang et al., 2007). Pemilihan polimer PEG sebagai bahan komposit dan pembuatan enkapsulan dikarenakan memiliki sifat yang baik bagi tubuh seperti biokompatibel, non-toksik, imunogenik, antigenik dan yang terpenting memiliki kelarutan yang tinggi di dalam air (Davidovich-Pinhas and Bianco-Peled., 2011). ...
p>Pengembangan penelitian tentang material berbasiskan sumber daya alam lokal dan dapat diperbaharui terus dikembangkan akhir-akhir ini. Hal tersebut didasari adanya kebutuhan material baru dengan karakteristik yang lebih menguntungkan dan dapat digunakan pada aplikasi yang spesifik. Penelitian ini bertujuan untuk mempelajari preparasi membran alginat-polietilen glikol (AP-PEG) dan aplikasinya sebagai enkapsulan. Alginat yang digunakan adalah hasil ekstraksi dari rumput laut cokelat Padina sp. Dengan metode maserasi jalur asam alginat. Preparasi membrane alginat Padina sp. -polietilen glikol (AP-PEG) dilakukan dengan perbandingan PEG-AP = 1:5; 1:10; 1:15; 0:1 (b/b). Analisis gugus fungsi terhadap seluruh membran yang dihasilkan, menunjukkan bahwa membran AP-PEG yang dihasilkan diprediksi sebagai hasil blending secara fisika karena tidak ada gugus fungsi baru yang terbentuk. Membran dengan perbandingan berat PEG-AP=1:15 memiliki karakteristik terbaik dengan persentase swelling sebesar 1465,5%, stress sebesar 14,588 MPa, strain 0,07 dan Modulus Young sebesar 193,13 MPa. Hasil analisis morfologi menunjukkan bahwa banyak rongga ditemukan pada membrane tersebut. Hasil uji disolusi terhadap membrane tersebut menunjukkan bahwa, pada pH 1,2 membran tersebut dapat melepaskan vitamin C sebesar 78,12% selama 60 menit dan tidak mengalami cracking . Di sisi lain, pada pH 7,2 membran tersebut dapat melepaskan vitamin C sebesar 83,54% dan cracking terjadi dalam waktu 12 menit. Hasil penelitian ini menunjukkan bahwa komposit AP-PEG dapat dibuat dari rumput laut coklat dan memiliki kemampuan sebagai enkapsulan.
Alginate Padina sp. - Polyethylene Glycol (AP - PEG) Membranes: Preparation, Characterization and Their Application as Encapsulant . The development of research on materials based on local and renewable natural resources has been continuously being developed recently. This is based on the need for new materials with more favorable characteristics and can be used in specific applications. This research aims to study the synthesis of alginate-polyethylene glycol (AP-PEG) membranes and their application as an encapsulant. The alginate was extracted from the brown seaweed Padina sp . by maceration method using alginic acid pathway. Alginate Padina sp. -polyethylene glycol (AP-PEG) alginate membrane was prepared with a ratio of PEG:AP = 1: 5, 1:10, 1:15 and 0:1 (w/w). The functional group analysis showed that the resulting AP-PEG membranes were predicted as a result of physical blending due to no new functional groups are formed. The membrane with a weight ratio of PEG:AP = 1:15 had the best characteristics, with a percentage of swelling of 1465.5%, stress of 14.588 MPa, 0.07 strain, and Young Modulus of 193.13 MPa. Morphological analysis showed that the membrane obtained had many cavities. The dissolution test showed that the AP-PEG membrane was able to release vitamin C of 78.12% for 60 minutes at pH 1.2 and no cracking was observed, while at pH 7.2 the membrane was able to distribute vitamin C by 83.54% and cracking occurs within 12 minutes. The results of this study indicate that AP-PEG composites can be made from brown seaweed and have good encapsulant capabilities.
... jiwa penduduk) (Kurnia, 2011), maka penatalaksanaan terapi ulkus lambung terkini harus digali dengan metode yang efektif dan efisien dengan penggunaan bahan alam sebagai sumber obat dan sebagai obat. Penelitian sebelumnya menunjukkan pemberian 1 mL sirup dapat menyembuhkan ulkus lambung tikus yang diinduksi dengan aspirin 400 mg/kgbb tikus (Arianto et al., 2014) dan pemberian fukoidan kepada pasien di Unit Endoskopi Rumah Sakit Cipto Mangunkusumo dapat menambah ketebalan mukus mukosa lambung pada pasien gastritis kronik (Renaldi et al., 2011). ...
Tujuan penelitian untuk mengetahui efek antiulkus isolat fukoidan dan Sargassum polycystum terhadap tikus putih jantan. Sampel terdiri dari 45 ekor tikus jantan dibagi 9 kelompok yaitu normal, CMC-Na, sukralfat, fukoidan dan 25mg/kgbb, 50mg/kgbb dan 100mg/kgbb. Perlakuan diberi per oral selama 10 hari. Pada hari ke-10, tikus dipuasakan selama 24 jam dan diberikan induksi etanol P.A. Kemudian tikus dikorbankan dan diambil lambung untuk dilakukan pemeriksaan makroskopik dan mikroskop. Hasil pemeriksaan karakteristik simplisia Sargassum polycystum diperoleh kadar air 9,05%, susut pengeringan 8,74% dan rendemen hasil isolasi fukoidan dan adalah 4,01% dan 6,4%. Hasil identifikasi fukoidan secara spektrofotometri FTIR menunjukkan bentuk spektrum dan kurva serapan identik dengan baku pembanding fukoidan. Persentase jumlah tukak masing-masing dosis fukoidan dan yaitu, dosis 25mg/kgbb (1.04 dan 0,85), dosis 50mg/kgbb (0,84 dan 0,67), dosis 100mg/kgbb (0,21 dan 0,40). Kesimpulan hasil penelitian adalah isolat fukoidan dan memiliki efek gastroprotektif terhadap lambung tikus putih dengan dosis optimum 100mg/kgbb.
... It is an anionic bioadhesive polymer, forming hydrogen bonds with hydroxyl group of polysaccharide chain in mucous glycoprotein and its chemical bond was non-covalent [15]. Previous study also reported the bioadhesive properties of alginate beads [16], [17]. Alginate interacts with organic diacidic base piperazine and calcium salts [18]. ...
... Then, the preparation was made as gastroretentive drug delivery system using alginate beads to increase the absorption of curcumin. Alginate beads are a mucoadhesive gastroretentive drug delivery system [16], [17]. It might be useful to prolong the residence time of preparation in the stomach so that increases the drug absorption. ...
... The mucoadhesive properties of alginate beads have been previously reported [12], [16], [17]. The mucosa lining of the stomach is rich in mucin, which contain an oligosaccharide chain with terminal sialic acid. ...
BACKGROUND: Treatment of gastric ulcer using turmeric extract is less effective because curcumin has low solubility and degraded in alkaline intestinal pH. Therefore, it is necessary to convert turmeric extract into turmeric solid dispersion to increase the dissolution of curcumin and the preparation is made in gastroretentive drug delivery system to improve the absorption of curcumin in the stomach. AIM: The aim of the study was to determine the anti-ulcer effect of gastroretentive drug delivery system of alginate beads containing turmeric extract solid dispersion compared to alginate beads containing turmeric extract (without solid dispersion) and negative control. METHODS: Turmeric powder was macerated with 96% ethanol for 8 days. The macerate was evaporated with a rotary evaporator at 50°C to obtain a concentrated extract. Turmeric extract solid dispersion was prepared by the solvent method using polyvinylpyrrolidone as a carrier. The turmeric extract solid dispersion was encapsulated with alginate gel by gelation method. The antiulcer test was performed on rats with gastric ulcer that induced by 0.6 N HCl solution. The ulcer healing was observed macroscopically and microscopically (histopathology). RESULTS: The results of observation on the treatment of rats gastric ulcer that induced by 0.6 N HCl showed the gastroretentive drug delivery system of alginate beads containing turmeric extract solid dispersion effective in healing the gastric ulcer compared to negative control. The effectiveness was statistically significantly different (p < 0.05). Alginate beads containing turmeric solid dispersion were slightly more effective than alginate beads containing turmeric extract, but the effectiveness was not statistically significant (p > 0.05). CONCLUSION: Alginate beads containing turmeric extract solid dispersion were effective in treatment of gastric ulcer in rats.
