Drug Particle Size Research Articles

Nanosuspensions as an approach for improved solubility and anti-Ichthyophthirius multifiliis activity of magnolol

Natural products have gained recognition as a valuable resource and have significant implications in the field of aquaculture. Nevertheless, the limited water solubility of drugs, leading to compromised bioavailability, has been a persistent challenge in the realm of pharmaceutical research. Magnolol as a natural product, the low solubility leads to limited activity against Ichthyophthirius multifiliis, which severely limits the application of magnolol. Nanosuspensions are considered to be an important strategy to improve the solubility and bioavailability of insoluble drugs. The purpose of this study is to fabricate nanosuspensions that can effectively improve the solubility and antiparasitic activity of magnolol. Magnolol nanosuspensions (MNs) containg Pluronic F68 as a stabilizer was prepared by the solvent-antisolvent precipitation method. The results of TEM, DSC and FTIR analysis showed that the surfactant attached to the surface of magnolol, and the nanosuspensions process significantly reduced the crystallinity and improved the solubility and dissolution rate of magnolol. The Central Composite Design was adopted to investigate the effects of independent variables viz. amount of temperature (A), the ratio of pluronic F68 to magnolol (w/w) (B), and churning time (C) on particle size (Y), obtaining optimum nanosuspensions with a size of 32.03 nm. Compared with free magnolol, the release rate of magnolol in 119 nm and 35 nm MNs was significantly improved, and the release rate of magnolol was increased from 28.13% to 58.45% and 85.70% within 60 min. Further, the antiparasitic activity of MNs was measured. The results showed the reduction in drug particle size leads to an enhancement in the insecticidal activity of magnolol. Altogether, this study proposes a promising strategy to enhance activity by increasing the solubility of natural products.

Fabrication of marizomib-loaded zeolitic imidazolate framework-8@manganese dioxide for promising drug delivery system of glioma cancer cells

Marizomib is a novel, irreversible, brain-penetrant pan-proteasome inhibitor with encouraging findings in preclinical models and early-stage clinical trials for patients with newly diagnosed and recurrent glioblastoma. Marizomib (MRZ)-loaded zeolitic imidazolate framework-8 (ZIF-8) and manganese dioxide (MnO2) (termed as MRZ-ZIF-8 @MnO2) nanoparticles, a smart-functional therapeutic system, were prepared for the treatment of glioma cancer. Fourier transforms infrared (FTIR) and transmission electron microscope (TEM) were used to assess the structural and morphology properties of drug-loaded ZIF-8-NPs. The findings demonstrated this drug delivery carrier's narrow and particle size distribution. The anticancer drug MRZ released from the NPs was measured. The cell viability of glioma cancer cells (C6 and U87) treated with NPs was established using the cell counting kit-8. The in vitro proliferation of drug-loaded ZIF-8-NPs was substantially increased than that of free MRZ and drug-loaded ZIF-8-NPs treated cells. In addition, The C6 and U87 cell morphological staining studies, such as dual staining (acridine orange/ethidium bromide, AO/EB) and nuclear staining (4′,6-diamidino-2-phenylindole, DAPI), ascertain that the drug-loaded ZIF-8-NPs stimulates the apoptosis in glioma cancer cell lines. The results of morphological changes show that a high apoptosis level was found with drug-loaded ZIF-8-NPs. Reactive oxygen species (ROS) and mitochondrial membrane potential (MMP) validate the apoptotic mode of cancer cell death via the MMP pathway. These findings suggest that the as-fabricated MRZ-ZIF-8 @MnO2-NPs with the synergetic anticancer drug might be applied to treat glioma cancer.

In-vivo Estimation of Optimized Floating Microspheres Design by QBD approach

In order to regulate its release, avoid repeated dosing, and consequently maximize bioavailability, it is essential to develop and construct floating microspheres of glipizide. According to Strubel et al., HPMC and EC were combined to form glipizide-loaded floating microspheres using a solvent evaporation technique. Drug loading, particle size, and percent drug release were used as response factors in the formulation optimization process, which took into account polymer concentration and stirring rate as independent variables.The bulk density, tapped density, flowability, and particle size of the formulation batches were all evaluated. Its in-vitro performance was assessed using the standard pharmacopoeal assays as well as other procedures, including yield (%), drug polymer compatibility (FTIR scan), and tapped density (%). Analysis of compressibility particle size, drug entrapment effectiveness, surface topography (SEM), and an in vitro release research. with a yield of 88.30±0.53%, an ideal drug loading of 85.50±0.55%, and a preferred buoyancy of 91.93±0.61%, tiny to big and spherical microspheres were created at 40°C using a 1:6 polymer, 2% Tween 80, and that temperature. The development of a stable emulsion and equally sized internal phase droplets was largely dependent on the emulsifying agent. A crucial element in the emulsification process is the propeller's stirring speed. Additionally, it influences the droplets' size and shape, which has an impact on the microspheres. The decision was made to incorporate stirring rate and polymer concentration as independent variables in the experimental design while keeping the other variables fixed as a result of the debate that was just had. Measurements of the hypoglycemic response brought on by oral administration were used to determine the in vivo effectiveness of the optimized batch in healthy normal Wistar rats (250–300gm).

A review on recent advantages and evaluation of microparticles and their applications

Microparticles are free spherical dust between 1 and 1000 microns made of synthetic, non-biodegradable, and non-biodegradable polymers. There are two types of microparticles: microcapsules and micro matrix. The main types of microparticles are magnetic microparticles, polymer microparticles, bio-adhesive microparticles, biodegradable polymer microparticles, synthetic polymer microparticles, floating microparticles, and radioactive microparticles. The advantage of microcarriers over nanoparticles is that they do not cross the 100 nm interstitium during lymphatic transport and therefore act locally. Toxic substances can be solidified in the form of micro-encapsulated and dried particles. Moreover, methods to characterize numerous physicochemical parameters like drug release, thermal properties, and particle size are introduced, along with new tests like in vitro leaching tests and floating tests.

Glycyrrhizic Acid-Lipid Framework Nanovehicle Loading Triptolide for Combined Immunochemotherapy.

Despite the acknowledged advantages of combined immunochemotherapy for tumor treatment, the high efficiency of co-delivery of these combined agents into the targeted tumor tissue is still challenging. Herein, based on a "three-birds-with-one-stone" strategy, a facile glycyrrhizic acid (GL)-lipid hybrid nanoplatform loading triptolide (TP/GLLNP) is designed to better address the dilemma. Differing from the traditional liposomes with dual-drug co-delivery NPs, GL with a cholesterol-like structure is primarily employed to construct the lipid membrane skeleton of the GL-based lipid nanoparticle (GLLNP), and then triptolide (TP) is readily loaded in the lipid bilayer of GLLNP. The fabricated GLLNP possessed similar drug loading efficacy, particle size, and storage stability; none of the hemolysis; even higher membrane fluidity; and lower absorbed opsonin proteins compared with the conventional liposomes. Compared to TP-loaded traditional liposomes (TP/Lipo), TP/GLLNP exhibits significantly enhanced cellular uptake, cytotoxicity, and apoptosis of HepG2 cells. In addition, GLLNP could ameliorate tumor immunosuppression by promoting tumor-associated macrophage polarization from M2 to M1 phenotype. Furthermore, enhanced retention and accumulation in the tumor area of GLLNP could be found. As expected, TP/GLLNP displayed synergistic anti-hepatocellular carcinoma efficacy in vivo. In conclusion, this study provides an inspirational strategy to combine the anti-HCC benefits of GL and TP using a novel dual-drug co-delivery nanosystem.

Nanogels as novel drug nanocarriers for CNS drug delivery.

Nanogels are highly recognized as adaptable drug delivery systems that significantly contribute to improving various therapies and diagnostic examinations for different human diseases. These three-dimensional, hydrophilic cross-linked polymers have the ability to absorb large amounts of water or biological fluids. Due to the growing demand for enhancing current therapies, nanogels have emerged as the next-generation drug delivery system. They effectively address the limitations of conventional drug therapy, such as poor stability, large particle size, and low drug loading efficiency. Nanogels find extensive use in the controlled delivery of therapeutic agents, reducing adverse drug effects and enabling lower therapeutic doses while maintaining enhanced efficacy and patient compliance. They are considered an innovative drug delivery system that highlights the shortcomings of traditional methods. This article covers several topics, including the involvement of nanogels in the nanomedicine sector, their advantages and limitations, ideal properties like biocompatibility, biodegradability, drug loading capacity, particle size, permeability, non-immunological response, and colloidal stability. Additionally, it provides information on nanogel classification, synthesis, drug release mechanisms, and various biological applications. The article also discusses barriers associated with brain targeting and the progress of nanogels as nanocarriers for delivering therapeutic agents to the central nervous system.

Spanlastic-laden in situ gel as a promising approach for ocular delivery of Levofloxacin: In-vitro characterization, microbiological assessment, corneal permeability and in-vivo study

The objective of this study was to encapsulate the antibacterial drug levofloxacin hemihydrate (LF) into spanlastics (SLs) followed by incorporation into gelrite in situ gel to enhance its antibacterial activity and sustain ocular delivery. A combination of Span 60 as main vesicle component and Tweens as an edge activator (EA) was used to prepare SLs using the thin film hydration method. A 32 factorial design was applied to study the effect of formulation variables (ratio of Span 60: EA and type of EA) on SLs characteristics (encapsulation efficiency (EE%), particle size (PS), zeta potential (ZP) and percentage of drug released). In-vitro antimicrobial study was conducted to determine the antibacterial activity of the optimized formula. Finally confocal laser scanning microscopy (CLSM) was applied to monitor SLs corneal penetration. The optimum formulation (F5), contains 240 mg Span 60 and 60 mg Tween 60 as EA. F5 exhibited EE% = 59.7 ± 4.2%, PS = 177.6 ± 1.8 nm, PDI = 0.27 ± 0.022 and ZP = -40.6 ± 0.68 mV. Furthermore, only 39.37 ± 0.72% of LF amount was released after 4 h compared to complete release from drug solution. The apparent permeation coefficient was (14.7 × 10−3 cm/h) compared to (9.7 × 10−3 cm/h) for LF solution. Moreover, F5 exhibited 200% and 100% increase in the antibacterial efficacy against Pseudomonas aeruginosa and Staphylococcus aureus respectively.

Kaalamega Narayana Chendhooram (KMNC): Standardization, Characterization, and Instrumental Analysis of a Potential Anti- Oral, Anti-Lung, and Anti-Prostate Cancer of Herbal Mineral Formulation (A Siddha Medicine for Oral, Lung, and Prostate Cancer)

Lack of drug standardization is the main obstacle preventing Siddha pharmaceuticals from being recognized more frequently in poorer nations. The current study also standardized a Siddha herbal-mineral creation of KMNC that indicated cervical cancer by investigating its physio-chemical. Fourier transforms infrared radiation properties. It was performed to produce evidence-based statistics about this new formulation and to give researchers helpful information. The drug particle size was determined by SEM examination. XRF analysis was used to determine the medication's component percentage. On-to-be nanometers indicate that the experimental drug may have effective drug delivery. The physicochemical characteristics also instrumental investigations of KMNC are discussed in this work as part of standardization by AYUSH Guidelines. This Indian medical system describes KMNC as a white powder containing herbs, metal, also mineral ingredients. The physio-chemical assessment's findings show that KMNC has a specific gravity of 0.927, a pH assessment of 7.8, also percentage of losses after 105 ? C 0.3±0.05568 %, and a total ash rate of 1.2%.

Projection of Target Drug Particle Size in Oral Formulations Using the Refined Developability Classification System (rDCS).

Dissolution limitations to oral absorption can occur if the time required for dissolution is longer than the transit time across the small intestine and/or if dissolution is slower than the drug's permeation through the gut wall. These limitations most often occur for poorly soluble drugs. A standard method for overcoming dissolution issues is to reduce the particle size of the (solid) drug. Building on the refined Developability Classification System (rDCS), this work establishes a novel set of equations with which the appropriate degree of particle size reduction needed to mitigate dissolution limitations to absorption can be calculated. According to the type of data available, the appropriate equation(s) for each situation can be applied. Three case examples are used to illustrate implementation of the equations: voriconazole, lemborexant and istradefylline. Although for voriconazole (rDCS Class I) target radius (rtarget) estimates indicate that particle size reduction is unnecessary, for lemborexant (rDCS Class I) a radius of ≤20 µm would be required to improve absorption. For istradefylline (rDCS Class IIb) the rtarget was approximately 12 µm. Results are commensurate with literature information for these three drugs, signaling that the equations are suitable for application to a wide variety of drug substances.

A Pegylated Liposome Loaded with Raddeanin A for Prostate Cancer Therapy.

Raddeanin A (RA), a potent triterpenoid extracted from Anemone raddeana Regel, has a moderate therapeutic effect on prostate cancer (PCa), correlating with serious biological toxicity. Therefore, a RA-loaded PEGylated liposome drug delivery system was devised in this study. Hydrogenated soybean phospholipids (HSPC), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-Polyethyleneglycol-2000 (sodium salt) (DSPE-PEG2k), cholesterol (CHO), and RA were utilised to prepare a RA-loaded liposome (LRA) drug delivery system via the thin film hydration technique., The drug loading content was confirmed by high performance liquid chromatography. Dynamic light scattering was employed to evaluate the drug's particle size and stability. Methyl tetrazolium, colony formation, and Western blot (WB) were used in vitro to elucidate the inhibitory effect and mechanism of LRA on prostate cancer cells. Finally, xenograft model was used to confirm the tumor-inhibiting efficacy, clarify the mechanism, and determine the biosafety in mice. LRA has stable physicochemical properties and a diameter of 173.5 15.3 nm. LRA inhibited the growth of prostate cancer cells in a dose- and time-dependent manner. LRA can substantially reduce the expression of AR and HMGB1, induce apoptosis, regulate the expression of cell cycle-related proteins in vitro and in vivo. The results of the biosafety tests demonstrated that LRA effectively reduced the adverse effects of RA. As a drug delivery system, LRA could effectively and safely inhibit the progression of prostate cancer.

Development of CO2-responsive supramolecular drug carrier system for potential application in anticancer treatment

A strategy to construct carbon dioxide (CO2)-responsive supramolecular drug delivery systems for effective cancer treatment was successfully confirmed using self-assembled supramolecular nanoparticles containing water-soluble terminal uracil-functionalized poly(ethylene glycol) (U-PEG) as a functional carrier and CO2-sensitive imidazole-functionalized rhodamine 6 G (I-R6G) as a potent anticancer agent. Owing to the high-affinity interactions between I-R6G and U-PEG, U-PEG can effectively encapsulate I-R6G and spontaneously co-assembles into spherical nanoparticles in water, which possess tunable drug loading contents and particle sizes, unique intense fluorescence features, and good structural stability and anti-hemolytic capacity in aqueous biological environments, as well as rapid, selective CO2-responsiveness and well-controlled CO2-responsive drug release. Cytotoxicity evaluations revealed I-R6G-loaded U-PEG nanoparticles exhibited highly selective cytotoxic activity towards cancer cells, without affecting normal cells. In addition, in CO2-rich media, I-R6G-loaded nanoparticles led to higher cytotoxicity at lower doses than I-R6G-loaded nanoparticles in pristine media or pristine I-R6G in CO2-rich media. Crucially, cellular assays confirmed the presence of CO2 in the culture media substantially increased selective cell internalization of the I-R6G-loaded nanoparticles by cancer cells, and subsequently promoted intracellular release of I-R6G from the disassembled nanoparticles and subsequent reaction of I-R6G with CO2, which ultimately resulted in more rapid induction of apoptotic cancer cell death than I-R6G-loaded nanoparticles in pristine media. Therefore, the introduction of the CO2-sensitive agent I-R6G within this self-assembled nanocarrier system is an essential factor that may provide a potential way to enhance efficacy and reduce the side effects of chemotherapy.

Exploring the Potential of Ketoprofen Nanosuspension: In Vitro and In Vivo Insights into Drug Release and Bioavailability

Low water solubility and high permeability present formulation challenges for drugs categorized as Biopharmaceutics Classification System (BCS) Class II, resulting in reduced bioavailability. This research focuses on addressing the solubility issues of BCS Class II drugs, including Simvastatin, Ketoprofen, griseofulvin, ibuprofen, ketoconazole, and carbamazepine, which exhibit high permeability but poor solubility. A potential strategy to improve the solubility and bioavailability of these drugs is the utilization of nanosuspensions.
 This study investigates the application of nanosuspension technology to enhance the solubility of Ketoprofen, a BCS Class II drug. By reducing the drug's particle size within the nanosuspension, solubility is improved, leading to increased bioavailability and optimized therapeutic efficacy. The research includes in vitro and in vivo experiments to evaluate the drug release profiles and bioavailability of Ketoprofen-loaded nanosuspensions.
 Significant findings from this research include the demonstration of improved bioavailability and enhanced drug release properties achieved with the nanosuspension formulation. In vitro studies show increased drug dissolution rates and improved release profiles compared to conventional formulations. In vivo experiments reveal enhanced pharmacokinetic parameters and therapeutic effectiveness of Ketoprofen when administered through the nanosuspension.
 These results highlight the potential of nanosuspensions as an efficient drug delivery system for BCS Class II drugs, addressing their solubility limitations and improving their bioavailability. The findings contribute to the development of novel strategies in pharmacology for enhancing drug solubility and therapeutic outcomes. Overall, this research emphasizes the significance of nanosuspension technology in optimizing the delivery of BCS Class II drugs and offers valuable insights for future formulation development and therapeutic applications.
 Keywords: Ketoprofen, Nanosuspensions, Ultrasonication, Precipitation, Dissolution rate, Oral bioavailability.

Synthesis of Glutathione-Responsive Cyclomatrix Polyphosphazene for Multimodal Theranostic Nanodrug Delivery

In this work, a multimodal (chemotherapeutic/photodynamic/photothermal) theranostic nanodrug delivery platform was developed based on the synergetic action of self-framed polyphosphazene prodrug and heptamethine cyanine dye IR-780. First, an electronegative glutathione (GSH)-responsive polyphosphazene prodrug abbreviated as HGEH was prepared via multicomponent condensation reaction of genistein (GEN), bis-(4-hydroxyphenyl)-disulfide, and hexachlorocyclotriphosphazene. The particle size of drug (GEN)-containing HGEH nanoparticles is adjustable. Subsequently, cationic near-infrared photosensitizer IR-780 was adsorbed onto the electron-rich HGEH to obtain the multimodal theranostic nanodrug delivery platform HGEH-IR780. The platform was demonstrated to retain high stability in avoiding drug leakage and enable controlled drug release in response to the tumor microenvironment, in which a higher GSH concentration exists. The in vitro experiments show that HGEH-IR780 undergoes photothermal and photodynamic processes to concurrently generate heat and reactive oxygen species for efficiently killing mouse breast cancer cells (4T1) upon exposure to a single-bandwidth near-infrared laser (808 nm). Specifically, HGEH-IR780 inhibits 4T1 cells by up to 80% at a concentration of 100 μg/mL. The as-developed HGEH-IR780 exhibits promising results in GSH-responsive anticancer activity and photodynamic/photothermal therapy, which provides a reference for the construction of the polyphenol flavonoid multimodal therapeutic nanoplatform.

Formulation and Characterization Sustained Release Mucoadhesive Microcapsule of Baclofen

Abstract: Background: Baclofen is used as skeletal muscle relaxant. Baclofen inhibit Polysynaptic and monosynaptic reflexes a hyperpolarisation. Baclofen drug absorbed rapidly and excreted in feces urine in unchanged form. Objectives: Aim of the current study was to formulate sustained release mucoadhesive microcapsules of Baclofen using different polymers like Chitosan, Carbopol934P, HPMC K4M. Materials and Methods: Ionotropic gelation method was used for preparation of microcapsules of baclofen. Dispersion of polymers and baclofen was dropwise added sodium tripolyphosphate solution to form microcapsule. The prepared microcapsules were evaluated for FTIR studies, micromeritic properties, drug entrapment efficiency, particle size and shape, SEM, swelling index, mucoadhesive strength, in vitro release studies. Results: Angle of repose of prepared microcapsules was in range 24.48 ± 1.39 to 38.08±1.67 showed good flowability. Prepared microcapsules showed bulk density in the range of 0.49±0.04 to1.22±0.06. All formulations showed Carr’s index and Hausner’s ratio in the range of 14.68 ±1.20 to 29.56 ± 1.97 and 1.16±0.012 to 1.25±0.016 respectively. Formulation F1 to F3 prepared with HPMC (K4M) showed drug release 77.78%, 74.94%, 77.99% and formulation F4 to F6 prepared with Carbopol 934P showed drug release 78.20%, 79.05%, 87.48% respectively in 12hr. Conclusion: Sustained release profile F6 formulation was obtained due to significant mucoadhesive efficiency of the Carbopol 934P. Hence the mucoadhesive microcapsules of Baclofen would be an effective strategy for the management of Muscle Pain. Keywords: Baclofen, Microcapsule, Carbopol 934P, HPMC K4M, Sustained Release.

Issues of Determining Particle Sizes of Various Drugs in Evaluating Their Quality

Issues of Determining Particle Sizes of Various Drugs in Evaluating Their Quality

Chitosan-grafted Microspherical Loaded In-situ Gels for Enhanced Transdermal Delivery of Roxithromycin: In-vitro/Ex-vivo Assessment

Background: Atleast once in life everyone experience different kinds of dermal diseases and the conventional dosage forms having a high rate of side effects. The discussed method is a better and alternative approach in case of patients’ compliance and sustained drug release. Objective: The objectives of this study are to prepare solid dispersion for enhancement of solubility of roxithromycin, encapsulation of solid dispersion into microspheres, decreased dose frequency, sustained release and incorporation of microspheres in in situ gel for easy utilization and adherence over the skin in microbial infection. Methods: Solid dispersion of roxithromycin and HPMC at a ratio of 1:1 was prepared by the melting method, and solubility was measured by in vitro dissolution rate. On the basis of 3² factorial design, 9 different formulations were evaluated by % drug release, particle size, and % entrapment efficiency. Lastly, in situ gel was prepared by a cold method, which was evaluated through gelling time and temperature; in vitro gelation method. Results: The solid dispersion was found to have a 1.3 times higher solubility than pure roxithromycin as proven by in vitro drug release. Whereas, microsphere MF-9 was selected as the best formulation via drug release (87.81%), entrapment efficiency (91.223%), % yield (86.681), and particle size (110μm). In-situ gel MIG-5 was selected as the best formulation on the basis of drug content (89.326±0.564), viscosity (9551.666±6.233), and gelling time (25.333±2.054). Conclusion: Solid dispersion was prepared successfully with higher solubility than the pure drug. Microspheres have shown sustained drug release and in situ gels have a good adhesive property and MIG-5 further enhances the sustained drug release behaviour.

Formulation and Development of Nanoparticulate System containing Rutin from Leaves Extract of Aegle marmelos for effective Management of Diabetes

Current work aimed at the modified release of content from carrier system at predetermined rate and secondly, to decrease the use of synthetic drug on biological system. Successive solvent extraction of crude drug of Aegle marmelos plant was done. Active constituent of leaves that is rutin was isolated and identified through HPTLC and FTIR. SLN was selected as carrier system and fabricated by solvent diffusion method. Characterization and performance evaluation of particulate system loaded with herbal plant extract of the Aegle marmelos leaves was done. TEM, In-vitro drug release profile, entrapment efficiency and particle size was determined. Solid lipid nanoparticles have enormous effect in loading high amount or loading dose concentration in body and also maintain the same over prolonged interlude of time. SLN was formulated and characterized for the particle size, shape and its distribution, percentage drug entrapment and In-vitro drug release profile along with the stability studies. In-vivo bio distribution studies on animals suggested the accumulation of formulations in the different organs. Solid lipid nanoparticles also show good stability as compared to other novel carrier systems. Prolonged release of natural drug from carrier system, decrease the dosing frequency and also decrease the dose size. Better results than marketed synthetic anti-diabetic drugs.

Nanosuspension: A Novel Technology for Drug Delivery

Nanotechnology includes nanosuspensions. Nanotechnology has become a huge area in the world of medicine. An appealing and promising approach to address the lipophilic like bio-available and poor solvability concerning the pharmaceuticals is nanosuspension. The majority of recently developed medications have poor water solubility. Drug formulation is usually complicated by medicines' limited water solubility. There are numerous standard methods for improving the solubility of pharmaceuticals that are poorly soluble, including Media Milling, Homogenization, precipitation technique, et cetera. A new approach in medication development is the development disintegrable medicinal formulations using nanotechnology. Particle sizes used in nanotechnology range are from 1 to 1000 nm. The increase in dissolving rate that results from drug particle size reduction into the submicron region naturally improves bioavailability. An efficient new method for improving the dissolution of low soluble in water medicines is nanosuspension technology. A nanosuspension improves the safety and effectiveness of a medicine by addressing issues with lipophilic like bio-available and poor solvability, as well as by changing the pharmacokinetics.

Vitexin loaded mixed polymeric micelles: preparation, optimization, evaluation and anti-osteoporotic effect

In this regard, we developed vitexin (Vi)-loaded D-ɑ-tocopherol polyethylene glycol succinate, polyvinylpyrrolidone K30 and sodium cholate mixed micelles (Vi-MMs) mainly for improving oral bioavailability and enhancing anti-osteoporotic effect of Vi. Thin layer dispersion method was employed to prepare Vi-MMs, and then the optimal prescription was optimized by the orthogonal design-response surface method, wherein encapsulation efficiency (EE) was used as optimizing index. The physical properties of Vi-MMs such as appearance morphology, particle size, and zeta potential were also characterized. We further analyzed the in-vitro release of Vi and Vi-MMs in three media and investigated the pharmacokinetics of Vi and Vi-MMs in rats. Anti-osteoporotic activity of Vi and Vi-MMs was assessed by establishing a zebrafish osteoporosis model with prednisone. Drug loading, EE, particle size and zeta potential of the optimized Vi-MMs were 8.58 ± 0.13%, 93.86 ± 1.79%, 20.41 ± 0.64 nm and −10 ± 0.56 mV, respectively. The optimized Vi-MMs were shaped spherically as exhibited by transmission electron microscopic technique, with evident core shell nano-structure, well dispersed. In all three media, the release rate of Vi-MMs was significantly higher than that of free Vi. The oral bioavailability of Vi-MMs was increased by 5.6-fold compared to free Vi. In addition, alleviation of prednisone induced osteoporosis in zebrafish by Vi-MMs further demonstrated good anti-osteoporotic effect. In summary, Vi-MMs exhibited enhanced bioavailability and anti-osteoporotic effect, which is expected to be potential nanocarrier for Vi applications in drug development.

Formulation and In-vitro evaluation of mometasone furoate mucoadhesive microsphere for pulmonary drug delivery

The purpose of the study was to develop and evaluate mucoadhesive microspheres of Mometasone for pulmonary drug delivery system having prolonged residence time and sustained drug release. Microspheres were prepared by emulsification solvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, In vitro mucoadhesion study and In vitro drug release studies. The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of 148 - 164μm, 68.0 - 85.0% and 67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms that formulation F5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed Mometasone mucoadhesive microspheres are promising for pulmonary drug delivery system.