Invitro Drug Release Profile Research Articles

Grewia asiatica Mucilage: A Smart Gelling Polymeric Material for Pharmaceutical Applications In Vitro Studies

Background: Natural plant-based materials have several advantages. They are biodegradable, biocompatible, non-toxic, cost-effective, environment friendly, easily available, and can undergo chemical modification. Objective: Grewia asiatica extracts contain various phytoconstituents and have therapeutic benefits such as antimicrobial and anti-diabetic properties. They form colloidal dispersions and make a highly viscous gel in water. Considering these properties of Grewia asiatica mucilage, the present work was aimed to investigate its application in the formulation of gel for the topical delivery of diclofenac sodium. Method: Gel formulations were prepared with and without penetration enhancers using 1% w/w diclofenac sodium as a model drug. The formulations were subjected to different evaluation tests like physical characterization, pH, spreadability, skin irritation, gel retrogradation, drug content and in vitro drug diffusion. The in vitro diffusion of the drug from different formulations was compared with the in vitro drug release profile of the marketed formulation (Omni gel, Cipla, India). To assess the release mechanism, the in vitro release data was analyzed using Korsmeyers-Peppas’ equation. Results: The mucilage showed good gelling behavior in 5.50, 5.75, 6.00, 6.25 and 6.50% concentrations. All the formulations followed the anomalous transport mechanism of drug release. The formulation BP3 showed 90% of drug release after 5.2h of dissolution study, which was similar to the marketed formulation. Hence, formulation BP3 was ideal among all the formulations. Conclusion: It might be concluded that, the Grewia asiatica mucilage may be used as a natural polymeric material for gel formulation.

Formulation development and evaluation of immediate release tablet of terbinafine hydrochloride

The immediate release tablet of antifungal drug Terbinafine hydrochloride were prepared developed and evaluated to increase solubility and bioavailability of low soluble drug by using wet granulation method. The tablets were prepared by varying concentrations and compositions of microcrystalline cellulose, sodium starch glycolate, hydroxyl propyl methyl cellulose, magnesium stearate, and colloidal silicon dioxide for seven trial batches. The drug excipient compatability study was studied by photostability study. No significant changes were observed in photostability study. The tablets were evaluated for disintegration test, content uniformity, and friability. Invitro drug release profile Terbinafine hydrochloride was examined in four different media PH0.1N HCL, PH4.5 acidic buffers, PH6.8 phosphate buffer and PH3.0 citrate buffer for 45 minutes. The drug release for trial batch no.7 shows 100.4% of drug release and innovator shows 102% of drug release. The formulation trial no 6 and 7 showed no significant changes during the study period of accelerated stability study for 3 months. The result of all formulation 7 showed that good developed formulation of immediate release tablet containing Terbinafine hydrochloride drug was similar to the marketed product with all respect and stable to effect of temperature and humidity.

Nanodelivery of doxorubicin for age-related macular degeneration

Objective: Polymeric nanoparticles (NPs) containing doxorubicin (DOX) were prepared for the inhibition of hypoxia-induced factor 1α (HIF-1α). Significance: HIF-1α is responsible for the upregulation of several angiogenic factors, including vascular endothelial growth factor (VEGF). DOX inhibits HIF-1α but is highly toxic. By encapsulating DOX in NPs, drug delivery will be sustained and toxicity will be reduced without limiting efficacy. Methods: DOX NPs were prepared using both polylactic coglycolic acid (PLGA) and chitosan. PLGA NPs were prepared via nanoprecipitation (NPC) and single and double emulsion diffusion (SE; DE). Chitosan NPs were formulated using ionic gelation (IG), and complex coacervation (CC). Size, polydispersity index (PDI), and zeta potential (ZP) were determined via dynamic light scattering (DLS) (n = 3). The encapsulation efficiency (EE), drug loading capacity (DLC) (n = 3) and in vitro drug release profiles (IVR) at 37 °C (n = 4) were analyzed via spectroscopy at 480 nm (λmax). The cytotoxicity of each formulation as well as free DOX solution in ARPE-19 cells was determined via MTT assay after 24 h (n = 3). HIF-1α and VEGF inhibition in ARPE-19 cells were measured via ELISA (n = 3). Results: The results were consistent with the hypothesis; the NP formulations decreased HIF-1α and VEGF-A expression in ARPE-19 cells with reduced cytotoxicity. SE, DE, and CC demonstrated low ZP as well as the most rapid drug release of the tested formulations. FTIR confirmed the presence of DOX on the SE NP surface, indicating instability. Conclusions: SE, DE, and CC destabilized. NPC was the most efficient formulation for the nanodelivery of DOX for AMD.

Anticancer Nano Formulation of Imatinib with Chitosan Polymer

Objective: Drug targeting is the capacity of the dosage form. In which the therapeutic agent acts specifically to desired site of action in the non-targeted tissue with the help of Nano particles is called as the drug targeting. IMATINIB is a used to treat cancer by chemo therapy. Cancers like chronic myeloid leukemia cancer (CML) and acute lymphoblastic leukemia cancer (ALL) and other specific types of gastrointestinal stromal cell tumor (GIST) systemic mast cell disease and Bone marrow failure disorder. It is administered by oral root. For ATP, Tyrosine kinase is act as a binding site. Methodology: The drug IMATINIB is loaded in the polymer chitosan, poly-(D) glucosamine is a bio compactible, bio degradable, nontoxic, antimicrobial and soluble in solvents. This preparation is done by emulsion-droplet coalescence method. Content of the Drug, Size of the particle and Zeta potential, Encapsulation efficiency and Drug release testing are described for this formulation in this study. Results: The Imatinib Nano particles were formulated and evaluated for its invitro drug release profile. Based on the invitro drug release profile of Imatinib nano particles formulation (INP1 – INP5) formulation INP3 was selected as the best formulation in which the particle size was 285.9nm. The invitro % drug release of INP3 formulation was 99.76 ± 0.82 and it was found to be the suitable formulation to manage the cancer. Conclusion: Hence it is concluded that the newly formulated controlled release nanoparticle drug delivery system of Imatinib may be idol and effective by allowing the drug to release continuously for 24 hrs.

Impact of Nanoparticulate Drug Delivery System of Herbal Drug in Control of Diabetes Mellitus

Aim: The main objective of the current study is to organize and evaluate polymeric nanoparticles for the selected drug Gymnemic acid, improve the bioavailability of poorly bioavailable gymnemic acid, enhance the anti-diabetic activity of Gymnemic acid, reduce the dose size of Gymnemic acid by reducing the particle size. Method and procedure: Gymnemic acid nanoparticles was prepared through emulsion-droplet coalescence method, by using chitosan polymer (GNP1-GNP5). Based on the invitro drug release profile of Gymnemic acid nanoparticles formulations (GNP1-GNP5) formulation GNP3 is selected as the best preparation in which the particle size was 195 nm[1]. Since from ancient times the naturopathic treatment for diseases has been explored widely and in advance momentum in the present situation, and has several pharmacological significance. Nano particulate drug delivery systems symbolize a promising drug delivery system[2] in recent years for its prescribed and targeted drug release. They exists as with a size choice of 10-1000nm, in which the drug or dissolved active ingredient, encapsulated, entrapped, absorbed or attached to the matrix system. The present research is a development of nanoparticulate[3,4] drug delivery system for Gymnema sylvestre by ionic gelation method. The formulation is characterized by particle size, zeta potential, particle morphology and best formulation was selected for the further studies. Result: The Gymnemic acid nanoparticles [1] were formulated and evaluated for its invitro drug release profile. The results showed that the in vitro drug release for GNP1, GNP2, GNP3, GNP4 and GNP5 were found 99.55± 0.89, 99.51± 0.34, 99.57± 0.31,78.82± 0.82 and 65.73± 0.62 respectively at the end of 24hrs. Conclusion: It can be concluded that the newly formulated controlled release nanoparticulate drug delivery[32] systems of Gymnemic acid may be ideal and effective in the treatment of diabetes mellitus by allowing the drug to release continuously for 24 hrs.

Biocompatible hydrogels for the controlled delivery of anti-hypertensive agent: development, characterization and in vitro evaluation

The aim of the present exploration was to develop novel pH-sensitive cross-linked Gelatin/Polyvinyl pyrrolidone hydrogels using different ratios of both the polymers and to investigate the effect of polymers and degree of crosslinking on dynamic, equilibrium swelling and invitro release pattern of the model drug (captopril). Grafting polymerization technique was used for the preparation of these hydrogels using glutaraldehyde as crosslinking agent. These polymeric materials were then used as model systems to envisage various important characterizations like FTIR (Fourier transform infrared spectroscopy), XRD (X-ray diffraction) and scanning electron microscopy (SEM). Phosphate buffers of pH 1.2, 6.5 and 7.5 were used for swelling and invitro drug release profile investigation. Different parameters like swelling analysis, porosity, sol-gel analysis, average molecular weight between crosslinks (Mc), solvent interaction parameter (χ), volume fraction of polymer (V2,s) and diffusion coefficient that affects the drug release behavior were also determined. Higher swelling and release was observed at lower pH values. FTIR spectra showed interaction between gelatin and polyvinyl pyrrolidone and successful formation of cross-linked structure. Pulsatile drug release study showed the controlled delivery of model drug. The release of drug occurred through non-fickian diffusion or anomalous mechanism. Aforementioned characterizations reveal successful formation of copolymer. pH sensitive swelling ability and drug release behavior suggest that the rate of polymer chain relaxation and the rate of drug diffusion from these hydrogels are comparable which also predicts their possible use for site specific captopril delivery.

Formulation and Evaluation of Pregabalin Loaded Eudragit S100 Nanoparticles

In this work, polymeric nanoparticles containing Pregabalin was prepared and optimized the ideal concentration of polymer based on its in vitro release profile for a period of 24hrs.The nanoparticles were prepared by solvent displacement method using various concentrations of Eudragit S100 (EPNP1-EPNP5). The prepared nanoparticles were characterized for its particle size, zeta potential, drug content, entrapment efficiency and invitro drug release profile. The preformulation study results confirmed the compatibility between the drug and other excipients used in the formulation. The optimized formulation was selected based on its particle size, entrapment efficiency and in vitro drug release profile. The formulation which contains 300mg of Eudragit S100 (EPNP5) was selected as optimized concentration for the controlled release of Pregabalin for a period of 24hrs.

Formulation of PLGA Polymeric Nanosuspension containing Pramipexole Dihydrochloride for improved treatment of Parkinson's Diseases

Aim and Objectives The present investigation was undertaken to develop nanosuspension of a hydrophilic drug pramipexole dihydrochloride and improve the entrapment efficiency of the drug. Materials and Methods: Nanosuspension of pramipexole dihydrochloride was prepared with PLGA and Pluronic F68 by the process of modified nanoprecipitation technique. The particle size, zeta potential, SEM, TEM and invitro dug release where performed. The cell viability study were performed by using SH-SY5Y cells. Result and Discussion: Nano-formulations are prepared with different concentrations of PLGA. The formulation variables such as polymer concentration (PLGA) were found to possess significant effect on the particle size and entrapment efficiency of drug in nanosuspension .The maximum entrapment efficiency, least particle size and optimal invitro drug release profile were exhibited with 1;3 ratio having 1% concentration of Pluronic F 68. The least particle size of 195 nm and maximum zeta potential value 34.8 mv were observed with PPNP 3 formulation. The SEM, TEM and invitro dug release of PPNP 3 were performed shows spherical shape with controlled release when compared to other formulations. Further the MTT assay were performed by using SH-SY5Y cells which shows more cell viability with PPNP 3 nanoformulation when compared to pure drug. Conclusion: PPNP 3 can be selected as best formulation among the other formulations. Thus, the biodegradable poly mer influences a better delivery in brain for the treatment in Parkinson’s disease

Controlled antibiotic-releasing Antheraea assama silk fibroin suture for infection prevention and fast wound healing

The quest for developing silk fibroin as a biomaterial for drug release systems continues to draw research interest owing to its impressive mechanical properties as well as biocompatibility and biodegradability. The aim of this study is to develop low-temperature O2 plasma-treated muga (Antheraea assama) silk fibroin (AASF) yarn impregnated with amoxicillin trihydrate as controlled antibiotic-releasing suture (AASF/O2/AMOX) for preventing postoperative site bacterial infection and fast wound healing. In this experimental study, AASF and AASF/O2/AMOX sutures are used to close the surgical wounds of adult male Wistar rats of 4months old and weighing 200-230g. Surface hydrophilicity induced by O2 plasma results in an increase in drug-impregnation efficiency of AASF/O2 yarn by 16.7%. Invitro drug release profiles show continuous and prolonged release of AMOX from AASF/O2/AMOX yarn up to 336hours. Invitro hemolysis assay reveals that O2 plasma treatment and subsequent impregnation of AMOX do not affect the heertetmocompatibility of AASF yarn. The AASF/O2/AMOX yarn proves to be effective for invitro growth inhibition of Staphylococcus aureus and Escherichia coli, whereas AASF offers no antibacterial activity against both types of bacteria. Invivo histopathology studies and colony-forming unit count data revealed accelerated wound healing activity of AASF/O2/AMOX over AASF yarn through rapid synthesis and proliferation of collagen, hair follicle, and connective tissues. Outcomes of this work clearly demonstrate the potential use of AASF/O2/AMOX yarn as a controlled antibiotic-releasing suture biomaterial for superficial surgical applications.