International Journal of Drug Delivery
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Controlled delivery of Imatinib mesylate from collagen coated poly(lactic acid) microspheres: In vitro release studies
Get PDFThe development of injectable microspheres for controlled drug delivery to the desired site is a major challenge. We demonstrated the possibility of entrapping an anticancer drug, Imatinib mesylate, in collagen coated biodegradable poly (lactic acid) microspheres with a mean diameter of 10-20 µm. The collagen coating on polymeric matrix surfaces through various surface modification techniques was the current scenario to improve bio-integration of the polymers with the in-vivo system. Here protein adsorption principle is used and various characterization techniques like FTIR, DSC and SEM analysis are used to confirm collagen coating. The reduction in burst release of the Imatinib from the PLA microspheres further confirms its presence and role in controlled release. This collagen coated PLA microspheres may have potential for the targeted delivery of Imatinib mesylate to treat gastrointestinal stromal tumors, chronic myeloid leukemia cancer
Two-Photon-Absorption Triggered Release of 5-Fluorouracil from Isomer-Pure Polymer Bound Syn-Head-to-Head Dimers for Novel Intraocular Lenses
Get PDFDifferent stereoisomers of the cytotoxic 5-fluorouracil (5FU) homodimers were synthesized by photochemical [2+2]-cycloaddition and polymerized into MMA/HEMA to form a novel drug-loaded copolymer for intraocular lenses as irradiation-activated treatment for secondary cataract. Three isomers were obtained, and showed significant differences in cleavage efficiency on photo-cleavage via single-photon-absorption (SPA) and two-photon-absorption (TPA). The most efficient TPA cleavage rate was observed for the syn-head-to-head 5FU dimer, which was, consequently, used for drug loading of the polymeric material to obtain a drug-loaded material of higher efficiency compared to previous works. The light and thermal stability of the polymer were confirmed and multi-dose release of the drug in aqueous solution for possible repeated treatment of cataract was proven
Modulation of in-vitro drug-release from a HPMC matrix system: Potential role of a disintegrant
Get PDFThe objective of the current study was to investigate the role of disintegrants in modulation of drug release from HPMC-based hydrophilic matrices. The polymer matrices of a water-soluble drug, Propranolol hydrochloride, were prepared in combination with different disintegrants by wet-granulation approach. The widely used superdisintegrants like crospovidone (CP), croscarmellose sodium (CCS), calcium carboxymethyl cellulose (CaCMC) and sodium starch glycolate (SSG) were investigated for their potential role as release modifiers. The polymer-disintegrant combinations were evaluated for in-vitro drug-release behaviour at various pH conditions coupled with determination of swelling behaviour and gel properties of matrices through texture analysis. The polymer-disintegrant combinations provided control over initial release rate and also exhibited complete drug release over 24 h. The work of penetration of hydrogels after 24 h dissolution study revealed that formulation with croscarmellose sodium showed complete relaxation of gel which fostered the complete drug release. Drug-release from the developed combination matrices was observed to be primarily Fickian diffusion based, except for combination of HPMC- sodium starch glycolate based matrices, where non-Fickian behaviour was observed. Barring sodium starch glycolate, all other polymer-disintegrant combinations provided pH-independent drug release. The accelerated stability studies of optimized HPMC-disintegrant matrix system were also satisfactory. The results of this study suggest that a suitable disintegrant when used in combination with HPMC, could modulate the drug-release and also synergize the release-controlling properties of hydrogel matrix systems. These findings can certainly be applied to develop controlled-release hydrogel matrix system of other highly water-soluble drug candidates, and hold a great potential in development of cost-effective and stable HPMC-matrix systems with customized drug-release behaviour.
Cross-linked Chitosan-Sodium Sulfate Matrix Systems Using Gel Casting Method for Sustained Drug Release of Doxorubicin Hydrochloride
Get PDFThe purpose of this study was to design a chitosan matrix systems made with cross-linking agents that targets control release of anticancer drug. Chitosan (CS) with cross-linking agent sodium sulfate (SS) was used for entrapping the model drug Doxorubicin Hydrochloride (DOX) through novel gel casting method. Scanning Electron Microscopy (SEM), Fourier Transforms Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), swelling index, drug entrapment efficiency and in vitro drug release studies were also done for physicochemical characterization of the formulations. Statistically significant different t50% and MDT values were noted between SS (5% w/v), SS (10% w/v) matrix systems and the control, as well as between SS (5% w/v) matrix systems and all the other formulations at pH 5.8 and pH 7.4. DOX release was slower in matrix systems without Explotab® and also at higher dissolution media pH (7.4). Statistically significant dissimilarity was observed between the control and the SS (5% w/v) f2 = 11.32±2.54; SS (10% w/v) f2 = 12.16±0.82 at pH 7.4. The findings of the study suggested that the matrix formulation is a promising carrier for DOX delivery
A comparative study of Okra gum on controlled release kinetics and other formulation characteristics of Tramadol HCl extended release matrix tablets Vs Synthetic hydrophilic polymers.
Get PDFThe main aim of this investigation was to develop a sustained release matrix tablets of Tramadol HCl using hydrophilic polymers such as hydroxyl propyl methyl cellulose (HPMC), in different grades (E15LV, K4M, K100M) and compare the various parameters against the natural polysaccharide Okra gum. The polymer proportions are used in different concentration in order to optimize the correct proportion of polymer to achieve controlled release profile. The matrix tablets were prepared by direct compression technique which is more industrially relevant. A small quantity of Carbopol was also incorporated in the formulation to give bio-adhesiveness & improved compression characteristics. The formulations were studied for pre-compression parameters and post-compression parameters. The in vitro drug release study was performed in 0.1N HCl (pH 1.2) for 1.5 hour and phosphate buffer (pH 6.8) were upto 12 hours. The study results revealed that the matrix tablet can be developed with the used polymers without any tablet manufacturing defects in optimized polymer concentration.. The polymers could control the drug release in various levels according to the concentration present in the formulation. The drug release profile was fitted with various pharmacokinetics models. The formulations showed the different degree of fit with different kinetic models. The drug release mechanism involves the combined process of diffusion, swelling and erosion
Preparation, optimization and in vivo evaluation of Eletriptan HBR fast dissolving oral films
Get PDFThe present investigation was aimed with the objective of developing fast dissolving oral films of Eletriptan HBr in order to attain quick onset of action for the better management of migraine attack. Twenty five formulations were prepared by solvent casting method using different polymer types, plasticizer types, surfactant concentrations and different ratio of hydroxypropyl methyl cellulose and maltodextrin. The prepared films were evaluated for folding endurance, thickness, drug content, in vitro/in vivo disintegration time, drug release and tensile test. The optimized formulation F17 containing HPMC 15cp and maltodextrin showed minimum in vitro disintegration time 11 seconds, highest dissolution rate i.e. 98.5% of drug within 10 min. The optimized film was further evaluated for bioavailability compared with a marketed product (Relpax-20mg). The pharmacokinetic results revealed that the fast dissolving oral films has higher peak blood concentration (Cmax, 0.455±0.1µg/ml) within shorter time (Tmax, 0.5 hours), indicating rapid absorption and faster onset of action with acceptable bioavailability value. Therefore, the oral fast dissolving film is considered to be potentially useful for the treatment of migraine disease where quick onset of action is desired, also improved patient compliance
Identification of Benzoxazolinone Derivatives Based Inhibitors for Depression and Pain Related Disorders Using Human Serotonin and Norepinephrine Transporter as Dual Therapeutic Target: A Computational Approach
Get PDFPain is commonly associated with depression. Both pain and depression share common biological pathways and neurotransmitters, which has implications for the treatment of both disorders. A drug that could ameliorate both pain and depression could be beneficial in the development of new therapeutics in the management of disorders associated with pain/depression dyad. Alterations in the neurotransmitters namely, serotonin and norepinephrine in the central nervous system (CNS) have been implicated in the pathophysiology of pain and depression. Serotonin and norepinephrine reuptake inhibitors (SNRIs) have been implicated as a novel therapeutic target for a wide range of biological functions, including pain, anxiety and depression. 2-benzoxazolinone (2-BOA) from the mangrove Acanthus ilicifolius and its derivatives have been reported for its analgesic and antidepressant activities. In the present work, docking studies were done on the crystal structure of human transporters of serotonin (hSERT) and on homology modeled human transporters of norepinephrine (hNET) as therapeutic targets of depression and pain related disorders using 2-BOA and its derivatives as potential candidates. A homology model for hNET was constructed using MODELLER and validated. Further docking studies were done on hSERT and hNET using 2-BOA and its structural analogs. The result of the study proposes the possible potential candidate among 2-BOA derivatives that may be further developed as a therapeutic lead compound for use in disorders associated with depression and pain
Fast dissolving oral films technology: A recent trend for an innovative oral drug delivery system
Get PDFOver the past few decades, there has been increased interest for innovative drug delivery system to improve the safety, efficacy and patient compliance, thereby increasing the product patent life cycle. In the recent years, many of the pharmaceutical groups are focusing their research on rapid dissolving technology. Fast dissolving oral films are the most advanced form of oral solid dosage form due to more flexibility and comfort. It improve the efficacy of APIs by dissolving within minute in oral cavity after the contact with less saliva as compared to fast dissolving tablets, without chewing and no need of water for administration. These films have a potential to deliver the drug systemically through intra-gastric, sublingual or buccal route of administration and also has been used for local action. This type of technology offer a convenient way of dosing medication, not to special population groups like pediatric, geriatric, bedridden patients, mentally ill patients, but also to the general population. Fast dissolving oral films are found to be satisfactory in many situations like allergic conditions, cold and cough, sore throat, nausea, pain, mouth ulcers, CNS disorders and CVS disorders. Oral film includes various ingredients for its formulation which includes polymers, active pharmaceutical ingredient, film stabilizing agents, plasticizers, sweeteners, flavours, colors, saliva stimulating agents, surfactants etc. The present review reflects information regarding formulation ingredients, technologies and evaluation tests employed in the preparation of fast dissolving oral films. However, for future growth point of view the fast dissolving oral films sector is well-positioned. It seems that the value of the overall oral thin films market will grow significantly
In vitro evaluation of six different mouthwashes against six oral pathogens
Get PDFDental caries and throat infections are still considered as serious public health problems and inflict a costly burden to health care services around the world and especially in developing countries. In the present study six mouthwashes were evaluated against six oral microorganisms using turbidity measurements and the antimicrobial effect of each mouthwash was detected by the agar well diffusion method. Of the six mouthwashes tested mouthwash A, B and C emerged as the most effective antimicrobial mouthwashes. Mouthwash C showed the highest effect at the concentrations 50% and 75% by the agar well diffusion method, against four of the oral microorganisms tested. K. pneumonia was the mostly affected bacteria showing the highest IZD after treatment with mouthwash C. TEM showed the effect of mouthwash C on K. pneumoniae as disruption of bacterial cell membrane and destruction of all internal cell contents. A combination between the most three effective mouthwashes A, B and C was done to investigate their synergestic or antagonistic effects compared to mouthwash C alone. It was surprising that the effect of mouthwash C alone was higher than the other tested combinations
Pharmacokinetic evaluation of newly developed isradipine sustained release formulation
Get PDFA specific and efficient method using High Performance Liquid Chromatography (HPLC) has been developed to validate the pharmacokinetics of sustained-release formulation containing Isradipine. The objective of the present study is to develop and validate PK of sustained release formulation containing Isradipine. The plasma samples of Isradipine were extracted using the protein precipitation technique (PPT). The detection wavelength of Isradipine, which was 325nm, was determined using UV spectrophotometer. Reversed phase Thermos c18 column was used for separation. 10mM ammonium acetate buffer (pH 4) and acetonitrile at a ratio of 20:80% v/v was used as the mobile phase with the flow rate of 1.0 ml/min. The linearity achieved in this method was in the range of 10-120 ng/ml. HPLC method provides extremely precise results and is an excellent and efficient method compared to others. The development of a sustained release formulation offers advantages such as prolonged blood levels of the drug and improved patient compliance. The formulated sustained release tablets containing Isradipine is capable of exhibiting sustained release properties, stable and feasible for industrial scale production. Thus they are capable of reducing the dose intake, minimize the blood level oscillations, dose related adverse effects, cost and ultimately improve the patient compliance in the hypertension