International Science Index
Mass Transfer of Paracetamol from the Crosslinked Carrageenan-Polyvinyl Alcohol Film
In this research, carrageenan extracted from seaweed Eucheuma cottonii was mixed with polyvinyl alcohol (PVA) and then crosslinked using glutaraldehyde (GA). The obtained hydrogel films were applied to control the drug release rate of paracetamol. The aim of this research was to develop a mathematical model that can be used to describe the mass transfer rate of paracetamol from the hydrogel film into buffer solution. The effect of weight ratio carrageenan-PVA (5: 0, 1: 0.5, 1: 1, 1: 2, 0: 5) on the parameters of the mathematical model was investigated also. Based on the experimental data, the proposed mathematical model could describe the mass transfer rate of paracetamol. The weight ratio of carrageenan-PVA greatly affected the amount of paracetamol absorbed in the hydrogel film and the mass transfer rate of paracetamol.
Formulation of Extended-Release Gliclazide Tablet Using a Mathematical Model for Estimation of Hypromellose
Formulation of gliclazide in the form of extended-release tablet in 30 and 60 mg dosage forms was performed using hypromellose (HPMC K4M) as a retarding agent. Drug-release profiles were investigated in comparison with references Diamicron MR 30 and 60 mg tablets. The effect of size of powder particles, the amount of hypromellose in formulation, hardness of tablets, and also the effect of halving the tablets were investigated on drug release profile. A mathematical model which describes hypromellose behavior in initial times of drug release was proposed for the estimation of hypromellose content in modified-release gliclazide 60 mg tablet. This model is based on erosion of hypromellose in dissolution media. The model is applicable to describe release profiles of insoluble drugs. Therefore, by using dissolved amount of drug in initial times of dissolution and the model, the amount of hypromellose in formulation can be predictable. The model was used to predict the HPMC K4M content in modified-release gliclazide 30 mg and extended-release quetiapine 200 mg tablets.
Formulation and in vitro Evaluation of Sustained Release Matrix Tablets of Levetiracetam for Better Epileptic Treatment
The objective of the present study was to develop sustained release oral matrix tablets of anti epileptic drug levetiracetam. The sustained release matrix tablets of levetiracetam were prepared using hydrophilic matrix hydroxypropyl methylcellulose (HPMC) as a release retarding polymer by wet granulation method. Prior to compression, FTIR studies were performed to understand the compatibility between the drug and excipients. The study revealed that there was no chemical interaction between drug and excipients used in the study. The tablets were characterized by physical and chemical parameters and results were found in acceptable limits. In vitro release study was carried out for the tablets using 0.1 N HCl for 2 hours and in phosphate buffer pH 7.4 for remaining time up to 12 hours. The effect of polymer concentration was studied. Different dissolution models were applied to drug release data in order to evaluate release mechanisms and kinetics. The drug release data fit well to zero order kinetics. Drug release mechanism was found as a complex mixture of diffusion, swelling and erosion.
Solid Dispersions of Cefixime Using β-Cyclodextrin: Characterization and in vitro Evaluation
Cefixime, a BCS class II drug, is insoluble in water but freely soluble in acetone and in alcohol. The aqueous solubility of cefixime in water is poor and exhibits exceptionally slow and intrinsic dissolution rate. In the present study, cefixime and β-Cyclodextrin (β-CD) solid dispersions were prepared with a view to study the effect and influence of β-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of cefixime was increased in the presence of β-CD and was classified as AL-type. Effect of variable, such as drug:carrier ratio, was studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR) and Differential scanning calorimetry (DSC). These studies revealed that a distinct loss of drug crystallinity in the solid molecular dispersions is ostensibly accounting for enhancement of dissolution rate in distilled water. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersions of cefixime showed a 6.77 times fold increase in dissolution rate over the pure drug.
Formulation and Evaluation of Niosomes Containing an Antihypertensive Drug
Niosomes were formulated with an aim of enhancing the oral bioavailability of losartan potassium and formulated in different molar ratios of surfactant, cholesterol and dicetyl phosphate. The formulated niosomes were found in range of 54.98 µm to 107.85 µm in size. Formulations with 1:1 ratio of surfactant and cholesterol have shown maximum entrapment efficiencies. Niosomes with sorbitan monostearate showed maximum drug release and zero order release kinetics, at the end of 24 hours. The in vivo study has shown the significant enhancement in oral bioavailability of losartan potassium in rats, after a dose of 10 mg/kg. The average relative bioavailability in relation with pure drug solution was found 2.56, indicates more than two fold increase in oral bioavailability. A significant increment in MRT reflects the release retarding ability of the vesicles. In conclusion, niosomes could be a promising delivery of losartan potassium with improved oral bioavailability and prolonged release profiles.
Polymeric Sustained Biodegradable Patch Formulation for Wound Healing
It is the patient compliance and stability in
combination with controlled drug delivery and biocompatibility that
forms the core feature in present research and development of
sustained biodegradable patch formulation intended for wound
healing. The aim was to impart sustained degradation, sterile
formulation, significant folding endurance, elasticity,
biodegradability, bio-acceptability and strength. The optimized
formulation comprised of polymers including Hydroxypropyl methyl
cellulose, Ethylcellulose, and Gelatin, and Citric Acid PEG Citric
acid (CPEGC) triblock dendrimers and active Curcumin. Polymeric
mixture dissolved in geometric order in suitable medium through
continuous stirring under ambient conditions. With continued stirring
Curcumin was added with aid of DCM and Methanol in optimized
ratio to get homogenous dispersion. The dispersion was sonicated
with optimum frequency and for given time and later casted to form a
patch form. All steps were carried out under strict aseptic conditions.
The formulations obtained in the acceptable working range were
decided based on thickness, uniformity of drug content, smooth
texture and flexibility and brittleness. The patch kept on stability
using butter paper in sterile pack displayed folding endurance in
range of 20 to 23 times without any evidence of crack in an
optimized formulation at room temperature (RT) (24 ± 2°C). The
patch displayed acceptable parameters after stability study conducted
in refrigerated conditions (8±0.2°C) and at RT (24 ± 2°C) up to 90
days. Further, no significant changes were observed in critical
parameters such as elasticity, biodegradability, drug release and drug
content during stability study conducted at RT 24±2°C for 45 and 90
days. The drug content was in range 95 to 102%, moisture content
didn’t exceeded 19.2% and patch passed the content uniformity test.
Percentage cumulative drug release was found to be 80% in 12h and
matched the biodegradation rate as drug release with correlation
factor R2>0.9. The biodegradable patch based formulation developed
shows promising results in terms of stability and release profiles.
Numerical Investigation of Thermally Triggered Release Kinetics of Double Emulsion for Drug Delivery Using Phase Change Material
A numerical model has been developed to investigate the thermally triggered release kinetics for drug delivery using phase change material as shell of microcapsules. Biocompatible material n-Eicosane is used as demonstration. PCM shell of microcapsule will remain in solid form after the drug is taken, so the drug will be encapsulated by the shell, and will not be released until the target body part of lesion is exposed to external heat source, which will thermally trigger the release kinetics, leading to solid-to-liquid phase change. The findings can lead to better understanding on the key effects influencing the phase change process for drug delivery applications. The facile approach to release drug from core/shell structure of microcapsule can be well integrated with organic solvent free fabrication of microcapsules, using double emulsion as template in microfluidic aqueous two phase system.
Preparation and in vivo Assessment of Nystatin-Loaded Solid Lipid Nanoparticles for Topical Delivery against Cutaneous Candidiasis
Solid lipid nanoparticles (SLNs) have gained great attention for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Our work deals with the preparation of nystatin loaded solid lipid nanoparticles (NystSLNs) using the hot homogenization and ultrasonication method. The prepared NystSLNs were characterized in terms of entrapment efficiency, particle size, zeta potential, transmission electron microscopy, differential scanning calorimetry, rheological behavior and in vitro drug release. A stability study for 6 months was performed. A microbiological study was conducted in male rats infected with Candida albicans, by counting the colonies and examining the histopathological changes induced on the skin of infected rats. The results showed that SLNs dispersions are spherical in shape with particle size ranging from 83.26±11.33 to 955.04±1.09 nm. The entrapment efficiencies are ranging from 19.73±1.21 to 72.46±0.66% with zeta potential ranging from -18.9 to -38.8 mV and shear-thinning rheological Behavior. The stability studies done for 6 months showed that nystatin (Nyst) is a good candidate for topical SLN formulations. A least number of colony forming unit/ ml (cfu/ml) was recorded for the selected NystSLN compared to the drug solution and the commercial Nystatin® cream present in the market. It can be fulfilled from this work that SLNs provide a good skin targeting effect and may represent promising carrier for topical delivery of Nyst offering the sustained release and maintaining the localized effect, resulting in an effective treatment of cutaneous fungal infection.
Extended Release System of Hypoglycemic Agent Containing Solid Dispersions: Strategies and Mechanisms
The main perspective of the present study aims at overcoming solubility problems by using the technique of solid dispersion. Repaglinide is a BCS Class II drug, having low aqueous solubility and therefore, low bioavailability. Solid dispersions of repaglinide with different carriers Polyvinyl Pyrrolidone (PVP) and Ethyl Cellulose (EC) in different ratios were prepared by suspending method and Dissolving methods. In vitro release studies revealed that the F7 formulation showed extended drug release. So, the dissolution profile of solid dispersion containing EC and PVP K30 (1: 3) was selected as the best formulation because of its extended drug release among all formulations. In conclusion, solid dispersions of Repaglinide in PVP have shown to be a promising approach to improve the bioavailability of Repaglinide.
New Coating Materials Based On Mixtures of Shellac and Pectin for Pharmaceutical Products
Shellac is a natural polyester resin secreted by insects. Pectins are natural, non-toxic and water-soluble polysaccharides extracted from the peels of citrus fruits or the leftovers of apples. Both polymers are allowed for the use in the pharmaceutical industry and as a food additive. SSB Aquagold® is the aqueous solution of shellac and can be used for a coating process as an enteric or controlled drug release polymer. In this study, tablets containing 10 mg methylene blue as a model drug were prepared with a rotary press. Those tablets were coated with mixtures of shellac and one of the pectin different types (i.e. CU 201, CU 501, CU 701 and CU 020) mostly in a 2:1 ratio or with pure shellac in a small scale fluidized bed apparatus. A stable, simple and reproducible three-stage coating process was successfully developed. The drug contents of the coated tablets were determined using UV-VIS spectrophotometer. The characterization of the surface and the film thickness were performed with the scanning electron microscopy (SEM) and the light microscopy. Release studies were performed in a dissolution apparatus with a basket. Most of the formulations were enteric coated. The dissolution profiles showed a delayed or sustained release with a lagtime of at least 4 h. Dissolution profiles of coated tablets with pure shellac had a very long lagtime ranging from 13 to 17.9 h and the slopes were quite high. The duration of the lagtime and the slope of the dissolution profiles could be adjusted by adding the proper type of pectin to the shellac formulation and by variation of the coating amount. In order to apply a coating formulation as a colon delivery system, the prepared film should be resistant against gastric fluid for at least 2 h and against intestinal fluid for 4-6 h. The required delay time was gained with most of the shellac-pectin polymer mixtures. The release profiles were fitted with the modified model of the Korsmeyer-Peppas equation and the Hixson-Crowell model. A correlation coefficient (R²)> 0.99 was obtained by Korsmeyer-Peppas equation.
Effect of Alginate and Surfactant on Physical Properties of Oil Entrapped Alginate Bead Formulation of Curcumin
Oil entrapped floating alginate beads of curcumin were developed and characterized. Cremophor EL, Cremophor RH and Tween 80 were utilized to improve the solubility of the drug. The oil-loaded floating gel beads prepared by emulsion gelation method contained sodium alginate, mineral oil and surfactant. The drug content and % encapsulation declined as the ratio of surfactant was increased. The release of curcumin from 1% alginate beads was significantly more than for the 2% alginate beads. The drug released from the beads containing 25% of Tween 80 was about 70% while a higher drug release was observed with the beads containing Cremophor EL or Cremohor RH (approximately 90%). The developed floating beads of curcumin powder with surfactant provided a superior drug release than those without surfactant. Floating beads based on oil entrapment containing the drug solubilized in surfactants is a new delivery system to enhance the dissolution of poorly soluble drugs.
Formulation and Characterization of Drug Loaded Niosomal Gel for Anti-Inflammatory Activity
The main aim of the present research was to encapsulate mefenamic acid in niosomes andincorporate the prepared niosomes in the carbopol gel base for sustained therapeutic action. Mefenamic acid loaded niosomes were prepared by thin film hydration technique and evaluated for entrapment efficiency, vesicular size and zeta potential. The entrapment efficiency of the prepared niosomes was found to increase with decreasing the HLB values of surfactants and vesicle size was found to increase with increasing the cholesterol concentration. Niosomal vesicles with good entrapment efficiencies were incorporated in carbopol gel base to form the niosomal gel. The prepared niosomal gel was evaluated for pH, viscosity, spreadability, extrudability and skin permeation study across the rat skin. The results of permeation study revealed that the gel formulated with span 60 niosomes sustained the drug release for 12h. Further the in vivo study showed the good inhibition of inflammation by the gel prepared with span 60 niosomes.
Novel Solid Lipid Nanoparticles for Oral Delivery of Oxyresveratrol: Effect of the Formulation Parameters on the Physicochemical Properties and in vitro Release
Novel solid lipid nanoparticles (SLNs) were developed to improve oral bioavailability of oxyresveratrol (OXY). The SLNs were prepared by a high speed homogenization technique, at an effective speed and time, using Compritol® 888 ATO (5% w/w) as the solid lipid. The appropriate weight proportions (0.3% w/w) of OXY affected the physicochemical properties of blank SLNs. The effects of surfactant types on the properties of the formulations such as particle size and entrapment efficacy were also investigated. Conclusively, Tween 80 combined with soy lecithin was the most appropriate surfactant to stabilize OXY-loaded SLNs. The mean particle size of the optimized formulation was 134.40 ± 0.57 nm. In vitro drug release study, the selected S2 formulation showed a retarded release profile for OXY with no initial burst release compared to OXY suspension in the simulated gastrointestinal fluids. Therefore, these SLNs could provide a suitable system to develop for the oral OXY delivery.
Development and Evaluation of Gastro Retentive Floating Tablets of Ayurvedic Vati Formulation
Floating tablets of Marichyadi Vati were developed with an aim to prolong its gastric residence time and increase the bioavailability of drug. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by wet granulation technique, using HPMC E50 LV act as Matrixing agent, Carbopol as floating enhancer, microcrystalline cellulose as binder, Sodium bi carbonate as effervescent agent with other excipients. The simplex lattice design was used for selection of variables for tablets formulation. Formulation was optimized on the basis of floating time and in vitro drug release. The results showed that the floating lag time for optimized formulation was found to be 61 second with about 97.32 % of total drug release within 3 hours. The vitro release profiles of drug from the formulation could be best expressed zero order with highest linearity r2 = 0.9943. It was concluded that the gastroretentive drug delivery system can be developed for Marichyadi Vati containing Piperine to increase the residence time of the drug in the stomach and thereby increasing bioavailability.
Effect of Polyvinyl Pyrrolidone and Ethyl Cellulose Concentration on Release Profile and Kinetics of Glibenclamide Extended Release Dosage Form System
The aim of present work was to optimize the effect of Ethyl Cellulose (EC) and Polyvinyl Pyrrolidone (PVP) concentration in extended release solid dispersion of Glibenclamide using combination of hydrophilic and hydrophobic polymers such as Polyvinyl Pyrrolidone and Ethyl cellulose. The advantage of solid dispersion technique provides a unique approach to particle size reduction and increased rates of dissolution. The compatibility studies of the drug and polymers were studied by TLC and results suggested no interaction between drug and polymers. Solid dispersions of Glibenclamide were prepared by common solvent evaporation method using Polyvinyl Pyrrolidone and Ethyl cellulose. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. F2 formulation prepared by solid dispersion method, displayed extended drug release followed by Higuchi matrix model indicating diffusion release of GLB from polymer matrices.
Dextran/Poly(L-histidine) Graft Copolymer for pH-Responsive Drug Delivery
pH-sensitive drug targeting using nanoparticles for
cancer chemotherapy have been spotlighted in recent decades. Graft
copolymer composed of poly (L-histidine) (PHS) and dextran
(DexPHS) was synthesized and pH-sensitive nanoparticles were
fabricated for pH-responsive drug delivery of doxorubicin (DOX).
Nanoparticles of DexPHS showed pH-sensitive changes in particle
sizes and drug release behavior, i.e. particle sizes and drug release rate
were increased at acidic pH, indicating that DexPHS nanoparticles
have pH-sensitive drug delivery potentials. Antitumor activity of
DOX-incorporated DexPHS nanoparticles were studied using CT26
colorectal carcinoma cells. Results indicated that fluorescence
intensity was higher at acidic pH than basic pH. These results
indicated that DexPHS nanoparticles have pH-responsive drug
Design of Salbutamol Sulphate Gastroretentive Nanoparticles via Surface Charge Manipulation
In the present study, development of salbutamol
sulphate nanoparticles that adhere to gastric mucus was investigated.
Salbutamol sulphate has low bioavailability due to short transit time in
gastric. It also has a positive surface charge that provides hurdles to be
encapsulated by the positively strong mucoadhesive polymer of
chitosan. To overcome the difficulties, the surface charge of active
ingredient was modified using several nonionic and anionic
stomach-specific polymers. The nanoparticles were prepared using
ionotropic gelation technique. The evaluation involved determination
of particle size, zeta potential, entrapment efficiency, in vitro drug
release and in vitro mucoadhesion test. Results exhibited that the use
of anionic alginate polymer was more satisfactory than that of
nonionic polymer. Characteristics of the particles was nano-size, high
encapsulation efficiency, fulfilled the drug release requirements and
adhesive towards stomach for around 11 hours. This result shows that
the salbutamol sulphate nanoparticles can be utilized for improvement
Packaging the Alkaloids of Cinchona Bark in Combination with Etoposide in Polymeric Micelles Nanoparticles
Today, cancer remains one of the major diseases that
lead to death. The main obstacle in chemotherapy as a main cancer
treatment is the toxicity to normal cells due to Multidrug Resistance
(MDR) after the use of anticancer drugs. Proposed solution to
overcome this problem is the use of MDR efflux inhibitor of cinchona
alkaloids which is delivered together with anticancer drugs
encapsulated in the form of polymeric nanoparticles. The particles
were prepared by the hydration method. The characterization of
nanoparticles was particle size, zeta potential, entrapment efficiency
and in vitro drug release. Combination nanoparticle size ranged 29-45
nm with a neutral surface charge. Entrapment efficiency was above
87% for the use quinine, quinidine or cinchonidine in combination
with etoposide. The release test results exhibited that the cinchona
alkaloids release released faster than that of etoposide. Collectively,
cinchona alkaloids can be packaged along with etoposide in
nanomicelles for better cancer therapy.
Pharmaceutical Microencapsulation Technology for Development of Controlled Release Drug Delivery systems
This article demonstrated development of
controlled release system of an NSAID drug, Diclofenac
sodium employing different ratios of Ethyl cellulose.
Diclofenac sodium and ethyl cellulose in different proportions
were processed by microencapsulation based on phase
separation technique to formulate microcapsules. The
prepared microcapsules were then compressed into tablets to
obtain controlled release oral formulations. In-vitro evaluation
was performed by dissolution test of each preparation was
conducted in 900 ml of phosphate buffer solution of pH 7.2
maintained at 37 ± 0.5 °C and stirred at 50 rpm. At predetermined
time intervals (0, 0.5, 1.0, 1.5, 2, 3, 4, 6, 8, 10, 12,
16, 20 and 24 hrs). The drug concentration in the collected
samples was determined by UV spectrophotometer at 276 nm.
The physical characteristics of diclofenac sodium
microcapsules were according to accepted range. These were
off-white, free flowing and spherical in shape. The release
profile of diclofenac sodium from microcapsules was found to
be directly proportional to the proportion of ethylcellulose and
coat thickness. The in-vitro release pattern showed that with
ratio of 1:1 and 1:2 (drug: polymer), the percentage release of
drug at first hour was 16.91 and 11.52 %, respectively as
compared to 1:3 which is only 6.87 % with in this time. The
release mechanism followed higuchi model for its release
pattern. Tablet Formulation (F2) of present study was found
comparable in release profile the marketed brand Phlogin-SR,
microcapsules showed an extended release beyond 24 h.
Further, a good correlation was found between drug release
and proportion of ethylcellulose in the microcapsules.
Microencapsulation based on coacervation found as good
technique to control release of diclofenac sodium for making
the controlled release formulations.
Chitosan/Casein Microparticles: Preparation, Characterization and Drug Release Studies
Microparticles carrier systems made from naturally occurring polymers based on chitosan/casein system appears to be a promising carrier for the sustained release of orally and parenteral administered drugs. In the current study we followed a microencapsulation technique based aqueous coacervation method to prepare chitosan/casein microparticles of compositions 1:1, 1:2 and 1:5 incorporated with chloramphenicol. Glutaraldehyde was used as a chemical cross-linking agent. The microparticles were prepared by aerosol method and studied by optical microscopy, infrared spectroscopy, thermo gravimetric analysis, swelling studies and drug release studies at various pH. The percentage swelling of the polymers are found to be in the order pH 4 > pH 10 > pH 7 and the increase in casein composition decrease the swelling percentage. The drug release studies also follow the above order.
Reproduction Performance of Etawah Cross Bred Goats in Estrus Synchronization by Controlled Internal Drug Release Implant and Pgf2α Continued by Artificial Insemination
The estrus female Etawah cross bred goats were
synchronized estrus by controlled internal drug release (CIDR)
implants for 10 days combined with PGF2α injection, and continued
by artificial insemination (AI) within the hours of 24 period. Vaginal
epithelium was taken to determine estrus cycle of the goats without
estrus synchronization. The estrus responds (the puffy of vulva and
vaginal pH) and percentage of pregnancy were investigated. The data
were analyzed descriptively and Independent Sample T-Test. The
results showed that the puffy of vulva and vaginal pH were
significantly different in synchronized estrus goats and control goats
(2.18 ± 0.33 cm vs. 1.20 ± 0.16 cm and 8.55 ± 0.63 vs. 8.22 ± 0.22).
Percentage of pregnancy was higher in synchronized estrus goats
(73.33%) than in control (53.3%). Estrus synchronization by using
CIDR implants and PGF2, continued by AI was effective to improve
reproduction performance of Etawah cross bred goats.