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1.
Int J Biol Macromol ; 270(Pt 1): 132306, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38740152

RESUMO

Combining natural polysaccharides with synthetic materials improves their functional properties which are essential for designing sustained-release drug delivery systems. In this context, the Aloe vera leaf mucilage/hydrogel (ALH) was reacted with acrylic acid (AA) to synthesize a copolymerized hydrogel, i.e., ALH-grafted-Polyacrylic acid (ALH-g-PAA) through free radical copolymerization. Concentrations of the crosslinker N,N'-methylene-bis-acrylamide (MBA), and the initiator potassium persulfate (KPS) were optimized to study their effects on ALH-g-PAA swelling. The FTIR and solid-state NMR (CP/MAS 13C NMR) spectra witnessed the formation of ALH-g-PAA. Scanning electron microscopy (SEM) analysis revealed superporous nature of ALH-g-PAA. The gel fraction (%) of ALH-g-PAA was directly related to the concentrations of AA and MBA whereas the sol fraction was inversely related to the concentrations of AA and MBA. The porosity (%) of ALH-g-PAA directly depends on the concentration of AA and MBA. The ALH-g-PAA swelled admirably at pH 7.4 and insignificantly at pH 1.2. The ALH-g-PAA offered on/off switching properties at pH 7.4/1.2. The metoprolol tartrate was loaded on different formulations of ALH-g-PAA. The ALH-g-PAA showed pH, time, and swelling-dependent release of metoprolol tartrate (MT) for 24 h following the first-order kinetic and Korsmeyer-Peppas model. Haemocompatibility studies ascertained the non-thrombogenic and non-hemolytic behavior of ALH-g-PAA.


Assuntos
Aloe , Hidrogéis , Mananas , Aloe/química , Concentração de Íons de Hidrogênio , Mananas/química , Hidrogéis/química , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Portadores de Fármacos/química , Polímeros/química , Porosidade , Resinas Acrílicas/química , Acrilatos
2.
Curr Pharm Des ; 30(1): 48-62, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38155469

RESUMO

Nanotechnology has emerged as the eminent focus of today's research to overcome challenges related to conventional drug delivery systems. A wide spectrum of novel delivery systems has been investigated to improve the therapeutic outcomes of drugs. The polymer-based nanocomposite hydrogels (NCHs) that have evolved as efficient carriers for controlled drug delivery are of particular interest in this regard. Nanocomposites amalgamate the properties of both nanoparticles (NPs) as well as hydrogels, exhibiting superior functionalities over conventional hydrogels. This multiple functionality is based upon advanced mechanical, electrical, optical as well as magnetic properties. Here is a brief overview of the various types of nanocomposites, such as NCHs based on Carbon-bearing nanomaterials, polymeric nanoparticles, inorganic nanoparticles, and metal and metal-oxide NPs. Accordingly, this article will review numerous ways of preparing these NCHs with particular emphasis on the vast biomedical applications displayed by them in numerous fields such as tissue engineering, drug delivery, wound healing, bioprinting, biosensing, imaging and gene silencing, cancer therapy, antibacterial therapy, etc. Moreover, various features can be tuned, based on the final application, by controlling the chemical composition of hydrogel network, which may also influence the released conduct. Subsequently, the recent work and future prospects of this newly emerging class of drug delivery system have been enlisted.


Assuntos
Sistemas de Liberação de Medicamentos , Polímeros , Humanos , Nanogéis , Disponibilidade Biológica , Polímeros/química , Hidrogéis/química
3.
Pharmaceutics ; 15(10)2023 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-37896205

RESUMO

The primary objective of this study was to assess the potential utility of quince seed mucilage as an excipient within a graft copolymer for the development of an oral-controlled drug delivery system. The Cydonia oblonga-mucilage-based graft copolymer was synthesized via a free radical polymerization method, employing potassium per sulfate (KPS) as the initiator and N, N-methylene bisacrylamide (MBA) as the crosslinker. Various concentrations of monomers, namely acrylic acid (AA) and methacrylic acid (MAA), were used in the graft copolymerization process. Metoprolol tartarate was then incorporated into this graft copolymer matrix, and the resultant drug delivery system was subjected to comprehensive characterization using techniques such as Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The swelling behavior of the drug delivery system was evaluated under different pH conditions, and in vitro drug release studies were conducted. Furthermore, pharmacokinetic parameters including the area under the curve (AUC), maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and half-life (t1/2) were determined for metoprolol-loaded hydrogel formulations in rabbit plasma, and these results were compared with those obtained from a commercially available product. The key findings from the study include observations that higher concentrations of acrylic acid (AA) and Cydonia oblonga mucilage (CM) in the graft copolymer enhanced swelling, while the opposite trend was noted at elevated concentrations of methacrylic acid (MAA) and N, N-methylene bisacrylamide (MBA). FTIR analysis confirmed the formation of the graft copolymer and established the compatibility between the drug and the polymer. SEM imaging revealed a porous structure in the prepared formulations. Additionally, the swelling behavior and drug release profiles indicated a pH-sensitive pattern. The pharmacokinetic assessment revealed sustained release patterns of metoprolol from the hydrogel network system. Notably, the drug-loaded formulation exhibited a higher Cmax (156.48 ng/mL) compared to the marketed metoprolol product (96 ng/mL), and the AUC of the hydrogel-loaded metoprolol was 2.3 times greater than that of the marketed formulation. In conclusion, this study underscores the potential of quince seed mucilage as an intelligent material for graft-copolymer-based oral-controlled release drug delivery systems.

4.
PLoS One ; 18(8): e0290223, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37607173

RESUMO

Prime objective of the current research was to develop a stable nimesulide emulgel with the help of arabinoxylan, a natural gelling agent extracted from Plantago ovata. The response surface methodology was used by a Design Expert 10 software to formulate and optimize the emulgel. The experimental design approach evaluated the impact of independent and dependent variables. Independent variables were different concentrations of arabinoxylan, span 80 and tween 20, whereas, dependent variables were viscosity, pH, and content uniformity. FTIR demonstrated the compatibility of nimesulide with the excipients. Stability study indicated no phase separation and no change in pH for formulation F1, F3 and F4. The negative values of zeta potential revealed the excellent stability of emulgel. Viscosity, spreadability and extrudability values were in desired range. Ex-vivo permeation study illustrated 86%, 55% and 66% release of the drug over a period of 24 h from the formulations F1, F3 and F4, respectively. Analgesic effect of the optimized emulgel was significantly higher in test group as compared to control and did not produce any sort of irritation. Therefore, it can be concluded that the newly developed emulgel based on arabinoxylan, as gelling agent, appear to be an effective drug delivery system.


Assuntos
Plantago , Excipientes , Movimento Celular , Géis
5.
Gels ; 9(6)2023 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-37367144

RESUMO

The present study was conducted to fabricate and characterize mucilage-based polymeric networks of Aloe vera for controlled drug release. Aloe vera mucilage was used to develop a polymeric network via the free-radical polymerization method using potassium persulphate as the initiator, N' N'-Methylene bisacrylamide as the crosslinker, and acrylamide as the monomer. Using varying concentrations of Aloe vera mucilage, crosslinker, and monomer, we developed different formulations. Swelling studies were conducted at pH 1.2 and 7.4. Concentrations of polymer, monomer, and crosslinker were optimized as a function of swelling. Porosity and gel content were calculated for all samples. FTIR, SEM, XRD, TGA, and DSC studies were conducted for the characterization of polymeric networks. Thiocolchicoside was used as a model drug to study the in vitro release in acidic and alkaline pH. Various kinetics models were applied by using a DD solver. Increasing content of monomer and crosslinker swelling, porosity, and drug release decreased while gel content increased. An increase in Aloe vera mucilage concentration promotes swelling, porosity, and drug release of the polymeric network but decreases gel content. The FTIR study confirmed the formation of crosslinked networks. SEM indicated that the polymeric network had a porous structure. DSC and XRD studies indicated the entrapment of drugs inside the polymeric networks in amorphous form. The analytical method was validated according to ICH guidelines in terms of linearity, range, LOD, LOQ, accuracy, precision, and robustness. Analysis of drug release mechanism revealed Fickian behavior of all formulations. All these results indicated that the M1 formulation was considered to be the best polymeric network formulation in terms of sustaining drug release patterns.

6.
RSC Adv ; 13(8): 4932-4948, 2023 Feb 06.
Artigo em Inglês | MEDLINE | ID: mdl-36762082

RESUMO

Herein, a drug delivery system (SSH-co-MAA) based on the mucilage from seeds of Salvia spinosa (SSH; polymer) and methacrylic acid (MAA; monomer) is introduced for the controlled delivery of venlafaxine HCl using a sustainable chemical approach. The optimized conditions for the designing of the ideal formulation (M4) of SSH-co-MAA were found to be 2.5% (w/w) of SSH, 30.0% (w/w) of MAA, 0.4% (w/w) of both N,N'-methylene-bis-acrylamide (MBA; cross-linker) and potassium persulfate (KPS; initiator). The structure characterization of SSH-co-MAA by Fourier transform infrared and solid-state CP/MAS 13C-NMR spectroscopy has confirmed the grafting of MAA onto SSH. The thermogravimetric analysis revealed that SSH-co-MAA is a stable entity before and after loading of the venlafaxine HCl-loaded SSH-co-MAA (VSSH-co-MAA). Scanning electron microscopy images of SSH-co-MAA after swelling then freeze drying showed the superporous nature of the hydrogel. The gel fraction (%) of SSH-co-MAA depended upon concentration of SSH, MAA, and MBA. The porosity (%) was increased with the increase in the concentration of SSH and decreased with the decrease in the concentration of MAA and MBA. The swelling indices, venlafaxine HCl loading, and release (24 h at the pH of the gastrointestinal tract) from VSSH-co-MAA were found to be dependent on the pH of the swelling media and the concentration of SSH, MAA, and MBA. The release of venlafaxine HCl followed non-Fickian diffusion mechanism. Conclusively, SSH-co-MAA is a novel material for potential application in targeted drug delivery applications.

7.
Pak J Pharm Sci ; 35(5): 1307-1319, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36451558

RESUMO

Present study was carried out to analyze the impact of three different monomers on release of losartan potassium from graft polymeric network prepared through free radical polymerization. N, N-methylene bis acrylamide was used as crosslinker and potassium persulfate as initiator. Losartan potassium as used as model drug because, it has very small plasma half-life and wide range of applications as an effective and efficient ARB (Angiotensin II Receptor Blockers) causing lower incidence of side - effects. Influence of three different monomers on swelling and in vitro drug release of the delivery system was evaluated at pH 1.2 and 7.4. The polymeric networks were characterized by Fourier transform infrared spectroscopy, Thermogravimetric analysis and Scanning electron microscopy. Polymeric network prepared with acrylic acid and methacrylic acid showed pH responsive behavior and while acrylamide based nexus exhibited pH independent style in swelling and drug release. However, among all the formulations, maximum swelling ratio (25.86) and optimal prolonged drug release (82.92%) was observed for GG-co-AA (M2) polymeric network at intestinal pH 7.4. The results indicated that GG-co-AA polymeric network could be an impending pH-sensitive drug delivery system for Losartan potassium. (M2) designated as formulation code with varying acrylic acid contents.


Assuntos
Antagonistas de Receptores de Angiotensina , Losartan , Inibidores da Enzima Conversora de Angiotensina , Polímeros , Acrilamidas
8.
Pak J Pharm Sci ; 35(2): 409-424, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35642395

RESUMO

The present study was conducted to fabricate and compare pH-sensitive polymeric networks of Artemisia vulgaris- Methacrylic acid using free radical polymerization conventional method and microwave-assisted method. Potassium persulphate and N' N'- Methylene bisacrylamide were employed as an initiator-crosslinker system. Swelling studies were performed at pH 1.2, 4.5, 6.8 and 7.4. Concentrations of polymer and monomer along with radiation dose were optimized as a function of swelling. Porosity and gel fraction were calculated for all samples. FTIR study confirmed the formation of cross-linked networks. Results of SEM indicated that the microwave irradiated polymeric network had a more porous structure. DSC and XRD study indicated the entrapment of drug inside the polymeric networks in amorphous form. In comparison to the conventional method, the polymeric network prepared by the microwave-assisted method exhibited high swelling ratios, porosity, thermal stability and drug release. These results signify microwave radiations as an effective alternative to the conventional heating method.


Assuntos
Artemisia , Liberação Controlada de Fármacos , Hidrogéis/química , Polímeros/química , Polissacarídeos
9.
Pharmaceutics ; 14(6)2022 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-35745795

RESUMO

The objective of this study was to fabricate and evaluate a pH sensitive cross-linked polymeric network through the free radical polymerization technique for the model drug, cyclophosphamide, used in the treatment of non-Hodgkin's lymphoma. The Hydrogels were prepared using a polymeric blend of agarose, Pluronic acid, glutaraldehyde, and methacrylic acid. The prepared hydrogels were characterized for drug loading (%), swelling pattern, release behavior, the ingredient's compatibility, structural evaluation, thermal integrity, and toxicity evaluation in rabbits. The new polymer formation was evident from FTIR findings. The percentage loaded into the hydrogels was in the range of 58.65-75.32%. The developed hydrogels showed significant differences in swelling dynamics and drug release behavior in simulated intestinal fluid (SIF) when compared with simulated gastric fluid (SGF). The drug release was persistent and performed in a controlled manner for up to 24 h. A toxicity study was conducted on white albino rabbits. The developed hydrogels did not show any signs of ocular, skin, or oral toxicity; therefore, these hydrogels can be regarded as safe and potential carriers for controlled drug delivery in biomedical applications.

10.
Gels ; 8(3)2022 Mar 09.
Artigo em Inglês | MEDLINE | ID: mdl-35323283

RESUMO

The aim of this study was to investigate the potential of Linum usitatissimum mucilage, a natural polymer, in developing a sustained release hydrogel for orally delivered drugs that require frequent dosing. For this purpose, nicorandil (a model drug)-loaded hydrogels with various feed ratios of Linum usitatissimum mucilage, acrylamide (monomer) and methylene bis-acrylamide (crosslinker) were prepared. The newly synthesized hydrogel formulations were probed fundamentally with respect to swelling behaviour, solvent penetration, and the release of the drug from the hydrogels. Later, the selected formulations were further characterized by Fourier-transform infrared spectroscopy, thermal analysis, X-ray diffraction analysis, and scanning electron microscopy. The swelling coefficient demonstrated a linear relation with the polymer ratio; however, an inverse behaviour in the case of monomer and crosslinker was observed. The drug release studies, performed at pH 1.2 and 4.5 and considering the dynamic environment of GIT, demonstrated that all formulations followed the Korsmeyer-Peppas model, displaying a slow drug release via diffusion and polymer erosion. FTIR analysis confirmed the successful grafting of acrylamide on linseed mucilage. Furthermore, scanning electron microscopy revealed a clear surface morphology with folds and pinholes in the hydrogel. Therefore, based upon the in-vitro outcomes, it can be concluded that a promising sustained release hydrogel can be prepared from natural polymer, Linum usitatissimum mucilage, offering many-fold benefits over the conventional synthetic polymers for oral delivery of drugs.

11.
Des Monomers Polym ; 25(1): 55-63, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35341118

RESUMO

The aim of this contemporary work was to formulate a controlled release mucoadhesive nanoparticle formulation for enhancing the oral bioavailability of Ticagrelor (TG), a BCS class IV drug, having low oral bioavailability of about 36%. The nanoparticles can act as efficient carriers for hydrophobic drugs, due to having high surface area and hence can improve their aqueous solubility due to their hydrophilic nature. The nanoparticles (NPs) of TG were formulated using chitosan (CH) as polymer and sodium tripolyphosphate (TPP) as cross-linker, by ionic gelation technique with varying concentrations of polymer with respect to TG and TPP. Characterization of prepared nanoparticles was carried out to assess zeta potential, size, shape, entrapment efficiency (EE) and loading capacity (LC), using zeta sizer, surface morphology and chemical compatibility analysis. Drug release was observed using UV-Spectrophotometer. By increasing concentration of CH the desired size of particles (106.9 nm), zeta potential (22.6 mv) and poly dispersity index (0.364) was achieved. In vitro profiles showed a controlled and prolonged release of TG in both lower pH-1.2 and neutral pH-7.4 mediums, with effective protection of entrapped TG in simulated gastric conditions. X-ray diffraction patterns (XRD) showed the crystalline nature of formed NPs. Hence, this effort showed that hydrophobic drugs can be effectively encapsulated in nanoparticulate systems to enhance their solubility and stability, ultimately improving their bioavailability and effectiveness with better patient compliance by reducing dosing frequencies as well.

12.
Des Monomers Polym ; 24(1): 351-361, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34912178

RESUMO

Natural mucilages are auspicious biodegradable polymeric materials. The aim of the present research work was to elucidate the characteristics of quince mucilage-based polymeric network for sustained delivery of metprolol tartrate and its toxicity evaluation. Mucilage was extracted by hot water extraction, and characterization of quince mucilage was accomplished by using Fourier transform infrared (FTIR) spectroscopy. Different batches of quince mucilage polymeric network were prepared by free radical polymerization by utilizing varying ratios of quince mucilage, acrylamide and crosslinker. Degree of swelling depends on concentration of mucilage, monomer and also on crosslinking density of polymeric network. FTIR illustrates proficient grafting, and morphological (scanning electron microscopy) analysis signified porous design. Hence, quince mucilage-based design was encouraging for sustained delivery of metprolol tartrate and acute toxicity evaluation proved that mucilage-based network was safe for oral drug delivery system.

13.
Int J Nanomedicine ; 16: 6345-6366, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34556985

RESUMO

BACKGROUND: Ticagrelor (TG), an antiplatelet drug is employed to treat patients with acute coronary syndrome, but its inadequate oral bioavailability due to poor solubility and low permeability restricts its effectiveness. PURPOSE: This contemporary work was aimed to design a novel pH-sensitive nanocomposite hydrogel (NCH) formulation incorporating thiolated chitosan (TCH) based nanoparticles (NPs) of Ticagrelor (TG), to enhance its oral bioavailability for effectively inhibiting platelet aggregation. METHODS: NCHs were prepared by free radical polymerization technique, using variable concentrations of chitosan (CH) as biodegradable polymer, acrylic acid (AA) as a monomer, N,N-methylene bisacrylamide (MBAA) as cross-linker, and potassium persulphate (KPS) as initiator. RESULTS: The optimum hydrogel formulation was selected for fabricating NCHs, considering porosity, sol-gel fraction, swelling studies, drug loading capacity, and TG's in vitro release as determining factors. Outcomes of the studies have shown that the extent of hydrogel swelling and drug release was comparatively greater at higher pH (7.4). Moreover, an amplifying trend was observed for drug loading and hydrogel swelling by increasing AA content, while it declined by increasing MBAA. The NCHs were evaluated by various physicochemical techniques and the selected formulation was subjected to in vivo bioavailability studies, confirming enhancement of bioavailability as indicated by prolonged half-life and multifold increase in area under the curve (AUC) as compared to pure TG. CONCLUSION: The results suggest that NCHs demonstrated a pH-responsive, controlled behavior along with enhanced bioavailability. Thus NCHs can be effectively utilized as efficient delivery systems for oral delivery of TG to reduce the risk of myocardial infarction.


Assuntos
Quitosana , Sistemas de Liberação de Medicamentos , Portadores de Fármacos , Liberação Controlada de Fármacos , Humanos , Hidrogéis , Concentração de Íons de Hidrogênio , Nanogéis , Ticagrelor
14.
Int J Nanomedicine ; 16: 4579-4596, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34267514

RESUMO

INTRODUCTION: The aim of current study was to prepare Linum usitatissimum mucilage (LUM) based nanoparticles, capable of encapsulating hydrophobic drug ezetimibe as nanocarriers. METHODS: Solvent evaporation and nanoprecipitation techniques were used to develop nanoparticles by encapsulating ezetimibe in the articulated matrix of polysaccharide fractions. Developed nanoparticles were characterized to determine the particle size, zeta potential, polydispersibility index (PDI), and entrapment efficiency (EE). Morphology and physicochemical characterization were carried out through SEM, FTIR, PXRD and thermal analysis. Saturation solubility and in vitro release studies were also performed. Safety assessment of ezetimibe loaded nanoparticles was evaluated via oral acute toxicity study. RESULTS: The mean particle size, zeta potential, PDI and EE for emulsion solvent evaporation were 683.6 nm, -28.3 mV, 0.39, 63.7% and for nanoprecipitation were 637.7 nm, 0.07, -27.1 mV and 80%, respectively. Thermal analysis confirmed enhanced thermal stability, whereas PXRD confirmed amorphous nature of drug. Saturation solubility (p-value <0.05) demonstrated improved solubility of drug when enclosed in linseed nanoparticles. Nanoprecipitation surpasses emulsion solvent evaporation in dissolution test by possessing smaller size. Acute oral toxicity study indicated no significant changes in behavioral, clinical or histopathological parameters of control and experimental groups. CONCLUSION: The in vitro release of ezetimibe was augmented by enhancing aqueous solubility through devised nanoparticles. Thus, linseed mucilage could act as biopolymer in the fabrication of nanoparticle formulation. The acute oral toxicological investigations provided evidence that LUMNs were safe after oral administration.


Assuntos
Portadores de Fármacos/química , Ezetimiba/química , Linho/química , Nanopartículas/química , Mucilagem Vegetal/química , Administração Oral , Ezetimiba/administração & dosagem , Tamanho da Partícula , Solubilidade
15.
Drug Deliv ; 28(1): 1093-1108, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34114907

RESUMO

In this work, series of pH-responsive hydrogels (FMA1-FMA9) were synthesized, characterized, and evaluated as potential carrier for oral delivery of an antiviral drug, acyclovir (ACV). Different proportions of ß-cyclodextrin (ß-CD), chitosan (CS), methacrylic acid (MAA) and N' N'-methylenebis-acrylamide (MBA) were used to fabricate hydrogels via free radical polymerization technique. Fourier transform infrared spectroscopy confirmed fabrication of new polymeric network, with successful incorporation of ACV. Scanning electron microscopy (SEM) indicated presence of slightly porous structure. Thermal analysis indicated enhanced thermal stability of polymeric network. Swelling studies were carried out at 37 °C in simulated gastric and intestinal fluids. The drug release data was found best fit to zero-order kinetics. The preliminary investigation of developed hydrogels showed a pH-dependent swelling behavior and drug release pattern. Acute oral toxicity study indicated no significant changes in behavioral, clinical, or histopathological parameters of Wistar rats. Pharmacokinetic study indicated that developed hydrogels caused a significant increase in oral bioavailability of ACV in rabbit plasma as compared to oral suspension when both were administered at a single oral dose of 20 mg kg-1 bodyweight. Hence, developed hydrogel formulation could be used as potential candidate for controlled drug delivery of an antiviral drug acyclovir.


Assuntos
Aciclovir/farmacocinética , Antivirais/farmacocinética , Quitosana/química , Hidrogéis/química , beta-Ciclodextrinas/química , Acrilamidas/química , Aciclovir/administração & dosagem , Aciclovir/efeitos adversos , Animais , Antivirais/administração & dosagem , Antivirais/efeitos adversos , Área Sob a Curva , Química Farmacêutica , Preparações de Ação Retardada , Relação Dose-Resposta a Droga , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Feminino , Concentração de Íons de Hidrogênio , Taxa de Depuração Metabólica , Metacrilatos/química , Coelhos , Ratos , Ratos Wistar , Propriedades de Superfície
16.
Drug Dev Ind Pharm ; 47(11): 1753-1763, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35282715

RESUMO

OBJECTIVES: This study was aimed to evaluate the toxicity profile of hydrogels of plant-derived mucilage from Aloe vera and Artemisia vulgaris used for various drug delivery applications, yet no such toxicity study has been reported for the toxicity evaluation of 3 D structures. New Drug carriers should be harmless for drug delivery applications. METHODS: Acute and sub-acute (repeated dose) oral toxicity studies were conducted following OECD 407 and 425 guidelines. In vitro toxicity through hemolysis and MTT assay were checked against RBC's and human macrophages respectively. RESULTS: The hemolysis and MTT assay showed good compatibility of hydrogels with blood components. Mutagenicity testing showed no genotoxic effects of hydrogels. In vivo toxicity evaluation was done in female albino rats and rabbits. General behavior, adverse effects, clinical signs and symptoms, and mortality were recorded for 14 days post-treatment which showed no significant (p < 005) abnormality. Hematological and biochemical parameters including LFTs and RFTs appeared to be normal with slight variations in the treated groups. The normal architecture of kidney, liver, heart and intestine was evident upon histopathological analyses. CONCLUSION: Hence, the results suggested that the 3 D structure of Aloe vera and Artemisia vulgaris based hydrogels are safe upon ingestion and can be used for drug delivery science being cheap, natural and biocompatible.


Assuntos
Aloe , Artemisia , Aloe/química , Animais , Materiais Biocompatíveis/toxicidade , Feminino , Hemólise , Hidrogéis/toxicidade , Extratos Vegetais/toxicidade , Coelhos , Ratos
17.
Drug Dev Ind Pharm ; 45(5): 754-766, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30640559

RESUMO

Current research work was conducted to synthesize Thiol modified arabinoxylan and its application in fabrication of hydrogel. Thioglycolic acid was esterified with arabinoxylan to prepare Thiolatedarabinoxylan. Appearance of peak at 2533.34 cm-1 in FTIR and thiol content showed successful thiolation. The pH-dependent Thiolatedarabinoxylan/acrylic acid (TAX/AA) hydrogels of perindopril erbumine were prepared via free-radical co-polymerization. Perindopril erbumine (PE) was employed as model drug. Different batches with different feed ratio of TAX, AA, and MBA were prepared and their influence on swelling, solvent penetration, and consequent drug release was investigated. Swelling coefficients increased with increase in pH. TAX/AA hydrogels were characterized by Fourier-transform infrared spectroscopy (FT-IR), Thermal Analysis (TA), X-Ray diffraction (XRD), and scanning electron microscope (SEM). Dissolution studies were performed at pH 1.2 and 7.4 in which drug release showed direct correlation with TAX and AA ratio. In vivo studies showed that Cmax of TAX-co-AA based hydrogel was 81.57 ± 0.35 ng/ml which was maintained for a longer time after its administration. All the results of in vivo studies were significant and TAX-co-AA based hydrogel enhances the bioavailability of perindopril erbumine.


Assuntos
Acrilatos/química , Portadores de Fármacos/química , Perindopril/farmacocinética , Xilanos/química , Animais , Disponibilidade Biológica , Liberação Controlada de Fármacos , Hidrogéis/química , Concentração de Íons de Hidrogênio , Perindopril/administração & dosagem , Plantago/química , Coelhos , Tioglicolatos/química , Xilanos/isolamento & purificação
18.
Pak J Pharm Sci ; 30(5): 1803-1814, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29084705

RESUMO

Lactic acid bacteria play vital roles in various fermented foods in Asia. This paper reviews many types of the world's lactic acid fermented foods and discusses the beneficial effects of lactic acid fermentation of food. The lactic acid bacteria associated with foods now include species of the genera Carnobacterium, Enterococcus, Lactobacillus, Lactococcus, Leuconostoc, Oenococcus, Pediococcus, Streptococcus, Tetragenococcus, Vagococcus and Weissella. Lactic acid bacteria (LAB) are involved in many fermentation processes of Asian traditional foods, demonstrating their profound effects on improving food quality and food safety. During the past few decades' interest has arisen in the use of the varied antagonistic activities of LAB to extent the shelf-life of protein-rich products such as meats and fish. This review article outlines the main types of LAB fermentation as well as their typical fermented foods such as idli, kishk, sauerkraut, koumiss, Suan-tsai, stinky tofu, Chinese sausage and kefir. The roles of LAB and the reasons for their common presence are also discussed.


Assuntos
Povo Asiático , Dieta/etnologia , Fermentação , Alimentos Fermentados/microbiologia , Microbiologia de Alimentos/métodos , Ácido Láctico/metabolismo , Lactobacillales/metabolismo , Ásia , Qualidade de Produtos para o Consumidor , Dieta/efeitos adversos , Alimentos Fermentados/efeitos adversos , Conservação de Alimentos/métodos , Qualidade dos Alimentos , Inocuidade dos Alimentos , Humanos , Valor Nutritivo
19.
Pak J Pharm Sci ; 30(1): 229-234, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28603137

RESUMO

The present report is a significant effort to explore detail description of N. Sativa, its pharmacognostic characteristics, morphological characteristics, and mechanism of actions, doses and medicinal uses. Nigella sativa (N. Sativa) is greatest form of healing medicine. It is also known as Prophetic Medicine as its use has been mentioned in Prophetic Hadit, as natural remedy for all the diseases except death. It is recommended on daily basis in Tibb-e-Nabwi (Prophetic Medicine). Hazrat Abu Hurairah States ''I have heard from Rasool Allah (PBUH) that there is cure for every disease in black seeds except death and black seeds are shooneeze''. Salim Bin Abdullah narrates with reference to his father Hazrat Abdullah Bin Omar that Rasool Allah (PBUH) said, 'Let all the black seed upon you, these contain cure of all diseases except death'. N. sativa claimed to have anti-inflammatory, analgesic, hepato-protective, neuro-protective, gastro-protective and other useful properties. Biological and pharmacological effects are attributed to its two important constituents Thymoquinone (TQ) and Nigella sativa oil (NSO). TQ has interaction with human serum albumin. Seeds containing volatile oils mainly Melanthin showed toxicity at larger doses. This report is a reference for all pharmaceutical researchers, physicians and biologists researching on N. sativa and will open a door towards novel agent.


Assuntos
Medicina Tradicional , Nigella sativa/química , Extratos Vegetais/uso terapêutico , Óleos de Plantas/uso terapêutico , Animais , Benzoquinonas/efeitos adversos , Benzoquinonas/isolamento & purificação , Benzoquinonas/uso terapêutico , Relação Dose-Resposta a Droga , História Antiga , Humanos , Medicina Tradicional/história , Fitoterapia , Extratos Vegetais/efeitos adversos , Extratos Vegetais/isolamento & purificação , Óleos de Plantas/efeitos adversos , Óleos de Plantas/isolamento & purificação , Plantas Medicinais , Sementes/química
20.
Acta Pol Pharm ; 74(2): 527-541, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29624258

RESUMO

A microwave induced irradiation synthesis, was proposed for the preparation of hydroxypropyl methylcellulose-graft-(polyvinylalcohal-co-acrylic acid) hydrogels. The hydrogels were separately synthesized by using microwave irradiation method and conventional water bath heating method. Moreover, the prepared hydrogels were loaded with an antihypertensive drug, captopril. Chemical groups, thermal stability and surface morphology of these hydrogels were characterized by FT-IR, DSC and SEM. Swelling ratios of the gels were measured gravimetrically at'pH 1.2 and 7.4. Results showed that micrographs obtained from scanning electron microscopy (SEM), revealed that gels synthesized using microwave irradiation had more uniformly porous network structures. The uniformity in porosity was due to rapid and instantaneous penetration of microwave energy throughout the surface and they had higher swelling ratios in comparison to hydrogels synthesized by water bath method. Thermal analysis (DCS and TGA) depicted that crosslinked polymers were more stable. FT-IR analysis had confirmed the formation of the new polymeric network. X-ray diffractogram revealed that crystallinity of HPMC was reduced in hydrogel prepared by microwave radiation. It had also been observed that high crosslinking density diminish swelling of hydrogel. A stable network of hydroxypropyl methylcellulose (HPMC), poly(vinylalcohal) (PVA) and acrylic acid was developed in shorter time period under influence of microwave radiations.


Assuntos
Acrilatos/síntese química , Anti-Hipertensivos/química , Captopril/química , Portadores de Fármacos , Micro-Ondas , Polímeros/síntese química , Tecnologia Farmacêutica/métodos , Compostos de Vinila/síntese química , Varredura Diferencial de Calorimetria , Química Farmacêutica , Cristalografia por Raios X , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Hidrogéis , Concentração de Íons de Hidrogênio , Microscopia Eletrônica de Varredura , Porosidade , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Propriedades de Superfície , Termogravimetria , Fatores de Tempo , Água/química
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