Topical 5-fluorouracil (5-FU) is used for the treatment of actinic keratosis and nonmelanoma skin cancer. Unfortunately, 5-FU per se shows a poor percutaneous permeation, thus reducing its anticancer effectiveness after topical administration. Therefore, we have constructed transfersomes, liposomes, and niosomes of 5-FU for topical applications in this investigation. Transfersomes were prepared by the solvent evaporation method, whereas liposomes and niosomes were constructed by reverse-phase evaporation method. The nanovesicles were characterized for particle size, shape, zeta potential, viscosity, entrapment efficiency, deformability, in-vitro permeation release, and kinetics and retention. Cytotoxicity study was carried out on HaCaT cells. Transfersomes (153.2 ± 10.3 nm), liposomes (120.3 ± 9.8 nm), and niosomes (250.4 ± 8.6 nm) were produced with a maximum entrapment efficiency of 82.4 ± 4.8, 45.4 ± 3.3, and 43.4 ± 3.2%, respectively. Moreover, transmission electron microscopy and atomic force microscopy assure the smooth and spherical shape of nanovesicles. Skin permeation and retention showed better permeability and retention than the nonvesiculized dosage form. The IC50 value of transfersomes (1.02 μmol/l), liposomes (6.83 μmol/l), and niosomes (9.91 μmol/l) was found to be far less than 5-FU (15.89 μmol/l) at 72 h. 5-FU-loaded transfersomes were found to be most cytotoxic on the HaCaT cell line in comparison with liposomes and niosomes. We concluded that vesiculization of 5-FU not only improves the topical delivery, but also enhances the cytotoxic effect of 5-FU. We have presented here a viable formulation of 5-FU for the management of actinic keratosis and nonmelanoma skin carcinoma.
CLC-HP-β-CD inclusion complex may potentially be used as a viable formulation of CLC.
Several studies have been conducted to establish the phenomenon of vaccine-drug interaction against various categories of chemotherapeutic agents, such as fluoroquinolones and chloramphenicol (1). They can either increase or decrease the phagocytic function or modulate the immune response triggered by an antigen (2). Investigations have revealed that chloroquine prophylaxis for malaria is associated with an impaired antibody response to rabies vaccine administered intradermally (3). It was proposed that chloroquine might interfere with the antigen processing mechanism and T-cell recognition (4, 5). In addition, chloroquine raises pH within lysosomes and thus interferes with the fusion of viral and lysosomal membranes, which is necessary to release viral nucleocapsid. It has been also shown that chloroquine interferes with secretion of interleukin-1 (IL-1) by monocytes, inhibiting the generation of immunoglobulin secretary lymphocytes (4). However, chloroquine did not affect the antibody response of yellow fever vac- Immune suppression resulting from chemoprophylaxis and potential drug interaction were investigated in experimental animals pre-medicated with ampicillin and chloroquine followed by immunization with bovine serum albumin bearing liposomes prepared by the reverse phase evaporation method. The prepared liposomes were evaluated for particle size, entrapment efficiency and in vitro release. Humoral immune response was measured in terms of systemic IgG antibody titre by the ELISA method. The present study showed that 7:3 molar ratio of soya phosphatidylcholine and cholesterol produced liposomes of mean diameter of 235.4 ± 10.3 nm and entrapment efficiency of 41.3 ± 3.2%. Ampicillin significantly (p < 0.05) decreased the antibody titre whereas chloroquine did not reduce the antibody titre significantly. The study will help in programming a new drug management and in characterization of vaccine-drug interaction.
Oral route is the most preferred route of drug administration due to its easy accessibility, intake, and wide range of choices making it economical. Currently, greater than 60% of marketed drugs are oral products. Over 90% of therapeutic compounds given orally areknown to possess oral bioavailability limitations. Therefore, there is a need to explore various approaches that can be used to improve oral drug bioavailability besides using physical and chemical means. The objective of this study is to prepare a formulation i.e. self microemulsifying drug delivery system (SMEDDS) of nifedipine with the intention to improve the increase dissolution rate (solubility). This will ensure the quick absorption and uniform bioavailability of nifedipine. Selection of oils, surfactants and co-surfactants was done by determining % transparency and on the basis of compatibility studies by FTIR spectra analysis. Different SMEDDS formulation were prepared of different ratio of oil:surfactantmix (1:9,2:8,3:7,4:6,5:5,6:4,7:3,8:2,9:1) and different ratio of surfactants : cosurfactants. Pseudo ternary phase diagram were constructed by water titration method to obtain a particle micro-emulsion region (on the basis of clarity and transparency). The formulation B-I was optimized because of maximum transparency (87.35%) and maximum % drug entrapment (95.32%). The average droplet size and zeta potential was found 86.05 and -0.189. The solubility of nifedipine increase in SMEDDS formulation upto72.17%.From in vitro dissolution study it was proved that SMEDDS formulation releases drug at faster rate, thus the objective of increase solubility and hence the better dissolution rate for uniform bioavailability via SMEDDS formulation of nifedipine was successfully achieved.
Objective: The objective of this research was to formulate bi-layer tablet which contains immediate-release layer of Paracetamol for quick onset of action and sustained release of Ibuprofen for prolonging long period. Materials and Methods: The following chemicals were used: Paracetamol (Combiotic Global Pvt. Ltd., India), Ibuprofen (Combiotic Global Pvt. Ltd., India), microcrystalline cellulose (MCC) (Avicel), and Polyvinylpyrrolidone (PVP) K-30 (Loba Chem). Wet granulation method was adapted to formulate the bilayer tablets. The immediate-release layer of Paracetamol was prepared using sodium starch glycolate as superdisintegrants, MCC as diluent, starch as binder. The sustained release layer of Ibuprofen was prepared using high-performance liquid chromatography E50LV and ethyl cellulose as binder along with other excipients such as MCC, PVP, and magnesium stearate by wet granulation technique. Result and Discussion: The release rate of Paracetamol from Formulations 1 was more than 80% at 40 min. In case of Ibuprofen, sustained-release polymers such as HPMC E50 LV were used to increase the release time. Conclusion: The bilayer tablets were prepared and show good release rate.
The objective of this study was to systematically conduct the process validation studies pertaining to the manufacturing activities of Bilayer tablet. The optimization of critical process steps and acceptance criteria at various stages of the process is referred in the validation report. The specifications of raw materials used in the manufacturing of Bilayer tablets of antihypertensive drugs have been derived from the monograph or previous history. The tolerance limits for the process parameters and the acceptance criteria for the various tests performed on in-process samples are derived from the FRND inputs. The physical characteristics of the final product are based on actual production scale, as some of these processes cannot be simulated in the laboratory. This research was carried out to produce a Bilayer tablet of antihypertensive drug. The immediate release Bilayer tablet of Telmisartan, Amlodipine besylate & Hydrochlorothiazide (40+5+12.5 mg) was successfully prepared. This combination Therapy indicated for the treatment of severe hypertension & coronary heart disease. Therefore, the purpose of performing optimization study for Antihypertensive drug form facility to provide necessary assurance for consistent quality product has been fulfilled. Keywords: Telmisartan, Amlodipine besylate, Bilayer tablet, Hydrochlorothiazide, optimization and validation.
Lipid nanocarriers are developed as an alternative to polymeric nanoparticles, liposomes and emulsions. NLCs are the second generation lipid carriers developed to overcome problems associated with Solid Lipid Nanoparticles and are utilized in various therapeutic approaches. NLCs were used for the delivery of lipophilic drugs .Biocompatible nature of lipids is responsible for its development as a good drug delivery. It was found to be having excellent characteristics over other lipid formulations.
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