Impact of various monomers on release of losartan potassium from guar gum based polymeric network.

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.

Development and evaluation of Artemisia vulgaris mucilage based polymeric network for controlled drug delivery.

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.

Aloe vera and artemisia vulgaris hydrogels: exploring the toxic effects of structural transformation of the biocompatible materials.

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.

Microbiological quality control of some non-sterile preparations commonly used in Pakistan.

The quality of medicines in some developing countries including Pakistan is not very satisfactory regarding safety and efficacy. In addition to sterile preparations, the microbial contamination of non sterile preparations should also be monitored according to USP microbial limits for these preparations. This study was designed to check the microbial quality of some commonly used non-sterile preparations available in Pakistan. Total 133 samples containing national and multinational brands of different dosage forms were collected from retail setups of Sargodha, Khushab and Chakwal cities. The total aerobic bacterial count and fungal contamination was tested by pour plate method. The absence of objectionable microorganisms was confirmed by using selective media, biochemical testing and microscopy. Bioburden of these preparations was also tested after a storage period of six months. The bio burden varied among all the selected non-sterile preparations whether of local or multinational brands. The highest load was observed in syrups, among which syrup number 1 showed maximum aerobic count (8.4×106). Lowest count was observed in tablets, among which tablet preparation number 1 contained 1.5×103aerobic bacteria. Creams and capsules produced no recovered bacteria. The fungal contaminants were also observed in all dosage forms except tablets. The isolated organisms included Gramnegative bacteria which contained objectionable ones such as Salmonella, Shigella, Pseudomonas and E.coli and some airborne moulds including Aspergillus spp., Penicillium spp., Fusarium spp. and Acremonium spp. Several measures such as GMPs, monitoring programs and SOPs should be followed by the pharmaceutical companies to reduce the microbial contamination level in the non sterile preparations. The regulatory agencies have to implement strict analysis strategy to check the microbial quality of the medicines before their release for sale in the market.

Phytochemical analysis and antimicrobial activity of aqueous and methanolic extracts of the flowers of Nelumbium speciosum.

In present investigation aqueous and methanolic extracts of Nelumbium speciosum flowers were screened for phytochemical constituents and antibacterial activity to ascertain their traditional use. Antimicrobial activity of both extracts was tested by Kirby-Bauer disc diffusion method against four Gram positive strains, viz. Staphylococcus aureus (ATCC25923), Streptococcus agalactiae (13813), Bacillus subtilis (ATCC 6633), Staphylococcus epidermidis (ATCC 12228) and four Gram negative bacterial strains Escherichia coli (ATCC 8739), Pseudomonas aeruginosa (ATCC 27853), Proteus mirabilis (12453) and Klebsiella pneumoniae (10031). Phytochemical analysis showed the presence of tannins, saponins and alkaloids in both extracts while flavonoids and steroids were present only in methanolic extract. Methanolic extract of Nelumbium speciosum flower showed concentration dependent antibacterial activity against all tested strains with maximum zone of inhibition (17.3±0.3mm) against P. aeruginosa. Aqueous extract showed concentration dependent activity against S. aureus, E. coli, B. subtilis and S. epidermidis with maximum antibacterial activity against E. coli (14.3±0.3mm). MIC of methanolic and aqueous extracts was in the range of 0.015-0.251 and 0.0625-0.251 mg/mL, respectively. Results showed that methanolic extract of Nelumbium speciosum exhibits superior antibacterial activity than aqueous extract.

Preparation and characterization of pH sensitive crosslinked Linseed polysaccharides-co-acrylic acid/methacrylic acid hydrogels for controlled delivery of ketoprofen.

Some pH responsive polymeric matrix of Linseed (Linum usitatissimum), L. hydrogel (LSH) was prepared by free radical polymerization using potassium persulfate (KPS) as an initiator, N,N-methylene bisacrylamide (MBA) as a crosslinker, acrylic acid (AA) and methacrylic acid (MAA) as monomers; while ketoprofen was used as a model drug. Different formulations of LSH-co-AA and LSH-co-MAA were formulated by varying the concentration of crosslinker and monomers. Structures obtained were thoroughly characterized using Fourier transforms infrared (FTIR) spectroscopy, XRD analysis and Scanning electron microscopy. Sol-gel fractions, porosity of the materials and ketoprofen loading capacity were also measured. Swelling and in vitro drug release studies were conducted at simulated gastric fluids, i.e., pH 1.2 and 7.4. FTIR evaluation confirmed successful grafting of AA and MAA to LSH backbone. XRD studies showed retention of crystalline structure of ketoprofen in LSH-co-AA and its amorphous dispersion in LSH-co-MAA. Gel content was increased by increasing MBA and monomer content; whereas porosity of hydrogel was increased by increasing monomer concentration and decreased by increasing MBA content. Swelling of copolymer hydrogels was high at pH 7.4 and low at pH 1.2. Ketoprofen release showed an increasing trend by increasing monomer content; however it was decreased with increasing MBA content. Sustained release of ketoprofen was noted from copolymers and release followed Korsmeyer-Peppas model.

Is folklore use of Euphorbia helioscopia devoid of toxic effects?

OBJECTIVE: To evaluate acute toxic effects of Euphorbia helioscopia in order to assure the safety and usefulness of herbal remedy. MATERIALS AND METHODS: The Organization for Economic Cooperation and Development (OECD) for chemical testing guidelines No. 425 for acute oral toxicity testing were followed in this study. Mice were divided into three groups (n = 5). Group I served as control. Groups II and III were administered methanol extract of E. helioscopia leaves and latex orally at dose of 2000 mg/kg, respectively. Then, all the animals were observed for two weeks. Blood sampling was done by cardiac puncture after 14 days from each group for biochemical analysis. Histopathology was performed to find out any microscopic lesion in vital organs. RESULTS AND DISCUSSION: LD50 was found greater than 2000 mg/kg. There was decrease in cholesterol, triglycerides, LDL and VLDL levels of latex and leaves with methanol extract-treated animals, with respect to control indicating plant's hypolipidemic effect. On macroscopic examination, no lesions were found on vital organs, such as liver, heart and kidney; and normal architecture was observed on microscopic examination. CONCLUSION: On the basis of results, it was concluded that methanol extract of E. helioscopia leaves and latex were devoid of toxic effects in acute toxicity study.

Acute toxicity studies of a novel excipient arabinoxylan isolated from Ispaghula (Plantago ovata) husk.

PURPOSE: The arabinoxylan from Ispaghula (Plantago ovata) husk has been proven scientifically as potential excipient. However, toxicity study of the arabinoxylan is still lacking. The present study was done to investigate the acute toxicity of arabinoxylan in two animal species. METHODS: The mice were exposed to (1 g/kg, 5 g/kg, 10 g/kg) and rabbits (2.5 g/kg, 5 g/kg) of arabinoxylan orally and observed for a period of 14 days. On day 15 hematology, serum biochemistry and necropsy was performed in mice relative organ weight calculated and histological examination was carried out. Primary dermal and eye irritation tests were carried out. Cardiac effects of isolated arabinoxylan were studied on frog heart. RESULTS: The acute administration of the arabinoxylan did not produce mortality or significant changes in, water and food consumption however body weights of mice and rabbits decreased initially with a gradual increase till day 14. Internal organs relative weights were found to be normal. Hematological biochemical and histopathological examination did not show any significant (p < 0.05) change. Primary dermal and eye irritation was not observed in treated rabbits. No change in heart rate and vascular contraction was observed in frog heart. CONCLUSION: This study has shown that acute administration of arabinoxylan may be safe.

Physicochemical characterization and evaluation of suspending properties of arabinoxylan from Ispaghula (Plantago ovata) husk.

The purpose of this study is to evaluate the use of arabinoxylan as potential suspending agent, an effective alternative to commercially used excipients for the preparation of pharmaceutical suspensions. Alkali extraction was done to separate arabinoxylan from ispaghula (Plantago ovata) seed husk by alkali extraction its physicochemical characterization was done and the suspending properties of arabinoxylan isolated were evaluated comparatively with those of bentonite at different concentration ranges of 0.125,0.25,0.5 and 1% in Zinc oxide suspension. The parameters employed for evaluation were sedimentation volume, degree of flocculation, flow rate, density, pH, redispersibility, microbiological evaluation and particle size analysis. Physicochemical characterization of arabinoxylan indicates its suitability as excipient as it has fair flow properties, low moisture content and almost neutral pH. Arabinoxylan at low conc. 0.125% showed sedimentation volume comparable to commercially used suspending agents such as bentonite 1% while suspensions containing higher concentrations such as 0.25% (sedimentation volume 92%), 0.5% (sedimentation volume 94%) and 1% conc. (sedimentation volume 98%) of arabinoxylan remained almost completely suspended during study period of 7 days. Formulations containing 0.125% and 0.25% arabinoxylan as suspending agents are easily redispersible as compared to bentonite containing formulation while formulation containing 0.5% arabinoxylan are moderately redispersible while formulation containing 1% suspending agent gel upon storage and was not redispersible. Furthermore arabinoxylan produces stable, highly flocculated suspension, which fulfilled microbiological, and particle size specifications, however the formulations containing higher arabinoxylan 1% concentration gel upon storage. So it is concluded that arabinoxylan could be used as effective suspending agent at low concentrations in Zinc oxide suspension.

Nanocomposite Hydrogels-A Promising Approach towards Enhanced Bioavailability and Controlled Drug Delivery.

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.

Appraisal of multifarious brands of Cephradine for their in vitro antibacterial activity against varied microorganisms.

The astounding and exceptional growth of generic pharmaceutical Industry in Pakistan has raised certain questions for drug regulatory authorities contemplating their efficacy and quality. The current study focuses on assessing the in-vitro antimicrobial activity of 24 brands of Cephradine 500mg capsules against 4 different strains by employing standardized methods. Disk diffusion method was performed on all brands to look into the susceptibility and resistance patterns. Standard disk of 5µg Cephradine powder were used during evaluation. The zones of inhibitions were ranged from 24-40mm against S. aureus, 24-40mm against E. coli, 20-25mm against K. pneumonia and 19-23mm P. mirabilis. On the basis of mean value, the multinational brands were found to have better zone of inhibitions and were better than local Pharmaceutical companies but ANOVA cooperative study showed that all brands of Cephradine showed similar comparable results. Further investigations by employing MIC method, quality of raw material with special emphasis on the shelf-life, excepients and method of manufacturing will be needed to obtain more authenticated results. The price of National and Multinational brands ranges from Rs.156.00-212.00 for 10 capsules. It is concluded that Public health is at risk because of noticeable growing widespread curse of the manufacture and trade of sub-standard or below par pharmaceuticals. The pecuniary accountability of management of pharmaceutical agents is additionally apparent. The results of the study need to be made public to boost the confidence of medical profession about the quality of locally manufactured pharmaceuticals. It will succour the foreign exchange being incurred on the trade in of medicines.

Exploring the gelling properties of Plantago ovata-based Arabinoxylan: Fabrication and optimization of a topical emulgel using response surface methodology.

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.

Aloe vera-Based Polymeric Network: A Promising Approach for Sustained Drug Delivery, Development, Characterization, and In Vitro Evaluation.

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.

Cydonia oblonga-Seed-Mucilage-Based pH-Sensitive Graft Copolymer for Controlled Drug Delivery-In Vitro and In Vivo Evaluation.

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.

Nephro-protective effect of vitamin C and Nigella sativa oil on gentamicin associated nephrotoxicity in rabbits.

Oxidative stress causes the generation of reactive oxygen species (ROS) that lead to nephrotoxicity. An aminoglycoside, gentamicin, has pronounced nephrotoxic effect in humans and animals and this study was planned to observe the nephro-protective effect of antioxidants, vitamin C and Nigella sativa oil. Serum creatinine, blood urea nitrogen, and antioxidant activity were measured as indicators of nephrotoxicity for all the groups of rabbits. Results showed that vitamin C and Nigella sativa oil both had nephro-protective effect as they lowered the values of nephrotoxicity indicators (serum creatinine, blood urea nitrogen, and antioxidant activity) as compared to gentamicin control group values. When these two antioxidants were given as combination, they proved to have synergistic nephro-protective effect.

Preliminary Investigation of Linum usitatissimum Mucilage-Based Hydrogel as Possible Substitute to Synthetic Polymer-Based Hydrogels for Sustained Release Oral Drug Delivery.

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.

Synthesis and evaluation of chitosan based controlled release nanoparticles for the delivery of ticagrelor.

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.

Formulation and Evaluation of Linum usitatissimum Mucilage-Based Nanoparticles for Effective Delivery of Ezetimibe.

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.

Fabrication, Characterization and Toxicity Evaluation of Chemically Cross linked Polymeric Network for Sustained Delivery of Metoprolol Tartrate.

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.

pH-Responsive Nanocomposite Based Hydrogels for the Controlled Delivery of Ticagrelor; In Vitro and In Vivo Approaches.

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.