Oral Administration Of Drug Research Articles

Replacing liquid with solid dosage forms in pediatric practice: Feasibility and economic impact from a hospital-based study

To identify the 10 drugs most frequently administered to children in liquid dosage forms which are eligible for replacement with suitable authorized solid dosage forms and to assess the expected economic impact of this substitution. The health record data from 312,152 oral drug administrations were analyzed. Ten drugs were selected according to their frequency of administration in liquid dosage forms, the availability of solid form alternatives, and the suitability of these alternatives for the children receiving the corresponding liquid forms. Potential hospital cost savings of the suggested substitutions were calculated. The 10 drugs identified as most frequently administered and for which suitable solid forms were available were: paracetamol, cyamemazine, valproic acid, clonazepam, furosemide, prazepam, hydroxyzine, alfacalcidol, amitriptyline, and levetiracetam. Thirty-four point six of the administrations of these drugs in liquid dosage forms could be delivered using suitable solid dosage forms without additional cost. Opportunities exist for substituting liquid dosage forms with market-available solid dosage forms suitable in size and dosage for the pediatric population.

Practical protocol for honey bee immobilization and oral administration of drugs and pathogens

Some fields in honey bee research require oral administration of substances to bees individually. This paper describes a relatively easy, practical, and reversible method for harnessing and oral feeding of honey bees. Individual bees are immobilized on a piece of balsa wood stick with two pins crossed on the junction between thorax and abdomen. Restrained bees can then easily be fed with a specific amount of chemical or pathogen in sucrose solution by inducing proboscis extension reflex. Important aspects and possible drawbacks of the method are also discussed.

In Silico-Based Experiments on Mechanistic Interactions between Several Intestinal Permeation Enhancers with a Lipid Bilayer Model.

Oral administration of drugs is generally considered convenient and patient-friendly. However, oral administration of biological drugs exhibits low oral bioavailability (BA) due to enzymatic degradation and low intestinal absorption. A possible approach to circumvent the low BA of oral peptide drugs is to coformulate the drugs with permeation enhancers (PEs). PEs have been studied since the 1960s and are molecules that enhance the absorption of hydrophilic molecules with low permeability over the gastrointestinal epithelium. In this study, we investigated the impact of six PEs on the structural properties of a model membrane using molecular dynamics (MD) simulations. The PEs included were the sodium salts of the medium chain fatty acids laurate, caprate, and caprylate and the caprylate derivative SNAC—all with a negative charge—and neutral caprate and neutral sucrose monolaurate. Our results indicated that the PEs, once incorporated into the membrane, could induce membrane leakiness in a concentration-dependent manner. Our simulations suggest that a PE concentration of at least 70–100 mM is needed to strongly affect transcellular permeability. The increased aggregation propensity seen for neutral PEs might provide a molecular-level mechanism for the membrane disruptions seen at higher concentrations in vivo. The ability for neutral PEs to flip-flop across the lipid bilayer is also suggestive of possible intracellular modes of action other than increasing membrane fluidity. Taken together, our results indicate that MD simulations are useful for gaining insights relevant to the design of oral dosage forms based around permeability enhancer molecules.

REVIEW STUDY ON ANALYSIS OF THE SOLUBILITY OF BIOPHARMACEUTICAL CLASSIFICATION SYSTEM CLASS II DRUGS IN A SELF-EMULSIFYING DRUG DELIVERY SYSTEM

By dissolving drug molecules in these solutions, a unit dosage form for oral administration can be generated for oral administration. Self-emulsifying drug delivery system (SEDDS) is utilized to address the inadequate bioavailability of poorly soluble and highly permeable drugs, according to the literature. These methods can disseminate and deliver hydrophobic medications as a unit dose form for oral administration in this fashion. SEDDS formulations self-emulsify (micro/nano) after being discharged into the intestinal lumen and coming into contact with the gastrointestinal (GI) fluid. Several factors must be considered to make the oral drug administration difficult, including poor water solubility and limited permeability. Self-emulsifying drug delivery can increase the solubility of biopharmaceutical classification system (BCS) II medicines. The SEDDS is a drug delivery system that enhances the solubility of lipophilic medications. It has risen in popularity over time. Under moderate agitation and subsequent dilution, GI fluids are categorized as hydrophilic liquid mixes that are isotropic. This research looks at a variety of uses as well as recent advancements in SEDDS composition, evaluation, dosage forms, and novel techniques to convert liquid SEDDS to solids. Final Thoughts Determining whether or not it is feasible to construct a BCS Category 2 medication formulation based on SEDDS represents a significant contribution of this effort. Medicines with solubility issues and low and variable bioavailability will benefit from the connected technologies.

Topical Administration of Drugs Incorporated in Carriers Containing Phospholipid Soft Vesicles for the Treatment of Skin Medical Conditions.

This review focuses on the improved topical treatment of various medical skin conditions by the use of drugs delivered from carriers containing phospholipid soft vesicles. Topical drug delivery has many advantages over other ways of administration, having increased patient compliance, avoiding the first-pass effect following oral drug administration or not requesting multiple doses administration. However, the skin barrier prevents the access of the applied drug, affecting its therapeutic activity. Carriers containing phospholipid soft vesicles are a new approach to enhance drug delivery into the skin and to improve the treatment outcome. These vesicles contain molecules that have the property to fluidize the phospholipid bilayers generating the soft vesicle and allowing it to penetrate into the deep skin layers. Ethosomes, glycerosomes and transethosomes are soft vesicles containing ethanol, glycerol or a mixture of ethanol and a surfactant, respectively. We review a large number of publications on the research carried out in vitro, in vivo in animal models and in humans in clinical studies, with compositions containing various active molecules for treatment of skin medical conditions including skin infections, skin inflammation, psoriasis, skin cancer, acne vulgaris, hair loss, psoriasis and skin aging.

Modified Montmorillonite as Drug Delivery Agent for Enhancing Antibiotic Therapy

The appealing properties of surfactant-intercalated Montmorillonites (Organo-montmorillonite, OMt) were successfully investigated to propose an effective drug delivery system for metronidazole (MNE) antibiotic therapy. This represents a serious pharmaceutical concern due to the adverse drug reactions and the low targeting ability of MNE. The non-ionic surfactant Tween 20 was used to functionalize montmorillonite, thus accomplishing the two-fold objective of enhancing the stability of clay dispersion and better controlling drug uptake and release. The adsorption process was performed under different experimental conditions and investigated by constructing the adsorption isotherms through high-performance liquid chromatography (HPLC) measurements. Powder X-ray diffraction (XRD) measurements were performed to characterize the MNE/OMt compounds. The gathered results revealed that the uptake of the drug occurs preferentially in the clay interlayer, and it is governed by positive cooperative processes. The presence of surfactant drives the adsorption into clay interlayer and hampers the adsorption onto external lamella faces. The good performances of the prepared OMt in the controlled release of the MNE were proved by investigating the release profiles under physiological conditions, simulating oral drug administration. Cytotoxicity measurements demonstrated the biocompatibility of the complexes and evidenced that, under specific experimental conditions, nanodevices are more biocompatible than a free drug.

Ayurveda approaches to COVID-19 in 2 wave: Lessons learned from practice

Ayurveda is a live traditional system of medicine with an unbreakable practice since 3000 years. Its principles and its approaches including oral administration of preventive drugs, herbs, formulae, decoction, indoor herbal medicine for fumigation, etc. were recommended for effective prevention and treatment whenever the emergent of new diseases. This paper highlights the patho-physiology of Corona as per Ayurveda, Clinical staging, preventive and curative approaches as learned time to time. and Anu taila nasya have excellent practice evidences for prevention of Covid-19 in 1 wave of corona. Sajeevani app developed by AYUSH to study the AYUSH practices. AYUSH -64 is an evidence-based treatment to cure mild to moderate COVID infection developed by Central Council for Research in Ayurveda Sciences. The second wave of COVID-19 is more tragedy than 1 wave and its impact on health care systems of our nation is devastating and unprecedented. National campaign for AYUSH-64 started and it is recommended in National Clinical Management Protocol based on Ayurveda and Yoga which is vetted by National Task Force on COVID management for COVID-19 Patients in Home Isolation. All Institute of Ayurveda released list of medicines for management of various symptoms of Covid. General public have more trusted upon Ayurveda practitioners as controversies of addition and deletion of steroid and antiviral in modern treatment protocol. The horror of Black (Mucormycosis) and white (Candiditis) fungus infection due to irrational use of immunosuppressive drugs confused the general people. More numbers of Covid patients received AYUSH-64 in 2 wave. Ayurveda Practice requires sound knowledge of Yukti Pramana(Logic and self judgement) by discerning clinical for better outcome irrespective of evidences and guidelines. We all are learning the pathogenesis of different mutants of Covid. Ayurveda approaches reduced the complication and progression of disease. This review will provide basic understanding Ayurveda for covid care.

Comparison of biomarker and chromatographic analytical approaches to pharmacokinetic study of sitagliptin.

The pharmacokinetic profiling of active compounds is necessary for drug development and application. Approaches to a pharmacokinetic study based on biological markers are alternatives to traditional approaches based on chromatographic methods. The aim of the study was to compare two analytical approaches to pharmacokinetics investigation for an example of sitagliptin in rabbits after one dose oral administration. The method for sitagliptin quantification in rabbit plasma samples based on a correlation between its concentration and dipeptidyl peptidase IV activity was proposed, validated, and applied. The high-performance liquid chromatography (HPLC)-ultraviolet (UV) method was also validated and applied for the same sample analysis. The plasma pharmacokinetics of sitagliptin after oral administrationto the rabbits in one dose was characterized after two analytical assays. Theclosevalues of the main pharmacokinetic parameters were obtained after two approaches. The nontraditional approach based on correlation of special marker activity and active substance concentration appears to be more sensitive than HPLC-UV. Thus, the sitagliptin concentrations determined by biomarker assay were higher than the lower limit of quantification (LLOQ) for a longer period (more timepoints) than after the HPLC-UV assay. This feature may influence the values of some calculated concentration-dependent (area under the curve [AUC]0-t , etc.) and time-dependent parameters (mean residence time [MRT], T1/2 , etc.). The values of Tmax obtained by the two approaches were similar and adequate for oral drug administration that confirms the correctness of biomarker selection for pharmacokinetics assessment. The obtained results on the example of sitagliptin confirms that the biomarker approach is adequate and applicable for a pharmacokinetics study. Similar approaches may be effective for individual compounds and complex mixtures when it is difficult or impossible to analyze them traditionally by chromatographic methods.

Hubungan Pengetahuan tentang Penggunaan OAD pada Pasien Diabetes Mellitus Tipe 2 terhadap Kepatuhan Penggunaan Obat Antidiabetes Oral di Puskesmas Singosari Malang

Abstract. Background: Diabetes Mellitus is a chronic disease characterized by high blood sugar levels in the body and can be caused by the pancreas not being able to produce enough insulin or because the cells in the body cannot respond to the insulin that has been produced. Management includes diet, physical activity, and administration of insulin injections and oral antidiabetic drugs (OAD). The objective of this study is to determine the relationship between knowledge of Type 2 Diabetes Mellitus patients and adherence to oral antidiabetic drug use at Singosari Public Health Center, Malang Regency. Research Methods: This research is analytic observational with a cross-sectional approach. Conducted in July 2021 at the Singosari Public Health Center, Malang Regency, by distributing questionnaires to 66 Type 2 Diabetes patients who met the inclusion criteria. The analysis was carried out with the SPSS application using descriptive and analytic methods. The results of the validity and reliability tests have met the requirements Result and Discussion:. Patients who have good knowledge of 74.2%, 18.2% good knowledge, and 7.6% poor knowledge. Patients with good knowledge were found to have 73% adherence to the use of OAD. Based on the results of the correlation test with Chi-Square, obtained a significant value of p = 0.000. Conclusion iit can be stated that there is a relationship between the knowledge of type 2 DM patients and adherence to the use of OAD at the Singosari Public Health Center, Malang Regency.

Mucoadhesive Microspheres of Atorvastatin Calcium: Rational Design, Evaluation and Enhancement of Bioavailability

Abstract: Background: Atorvastatin Calcium (ATC) used for lowering the cholesterol levels in body. It is competitive inhibitor of hydroxyl methylglutaryl-coenzyme A (HMG-CoA) reductase, followed mevalonate pathway, which have low bioavailability and poor solubility. Present work focus on development of mucoadhesive microspheres of atorvastatin calcium, for improve the delayed transit, continuous longer period release and preclinical pharmacokinetic estimation in rabbit. Materials and Methods: Microsphere was prepared by emulsification method in which the independent variables (like polymer amount) were studied on critical quality attributes like entrapment efficiency, percentage yield and in-vitro release. Microspheres were characterized in terms of physicochemical parameters, micromeritic properties, FT-IR, DSC and mucoadhesive wash-off test and further, evaluated for their pharmacokinetics study in rabbits. Results: The designed microsphere exhibited an average size with smooth surface, negative zeta potential, maximum entrapment efficiency and sustained release. Microspheres fulfil the micromeritic properties and showed no any interaction between drug and polymer, confirmed by FT-IR and DSC. The in-vivo study demonstrated that the prepared microspheres are effective for colon targeted drug delivery system at longer duration. In pharmacokinetics study, relatively steady plasma drug concentrations were observed within after oral administration of drug. The AUC0-24h for formulation were significantly higher than that of pure drug (p<0.05). Conclusion: The pre-clinical oral bioavailability study of drug was increased as the relative availability values were high compared with pure drug and it showed delayed transit for longer period of time. Key words: Atorvastatin calcium, Mucoadhesive, Microspheres, Colon targeting, Bioavailability.

Smart ingestible devices: Orally delivering macromolecules and beyond

Oral administration of macromolecule drugs is traditionally challenging due to the harsh environment these drugs navigate through the gastrointestinal tract and the resultant low blood adsorption. Recently, a series of work has demonstrated the use of smart ingestible devices comprising an intricate design of a drug-loaded vehicle that can adjust direction and accurately pierce into tissue wall, thus delivering macromolecule drugs with high efficiency.

In vitro and in vivo Anti-Toxoplasma Effects of Allium sativum Essential Oil Against Toxoplasma gondii RH Strain.

BackgroundSince no effective vaccine has been developed for toxoplasmosis, prophylaxis in seronegative pregnant women and immunocompromised patients with a CD4 <100 cells/μL is highly recommended as an ideal strategy to prevent this disease. This study aimed to assess the chemical composition, in vitro, and in vivo effects of Allium sativum essential oil (ASEO) against Toxoplasma gondii RH strain.MethodsThe in vitro anti-Toxoplasma effects of different concentrations of ASEO (32.5, 75, 150 µg/mL) were measured by MTT assay for 0.5, 1, 2, and 3 h. Male Balb/c mice were orally administrated ASEO at the doses of 200, 400, and 600 µg/kg/day for 14 days. One day after the completion of oral drug administration, the mice in all groups were infected intraperitoneally with 1×104 tachyzoites. They were checked daily and the rate of survival was recorded. The peritoneal fluids of the mice were collected and the mean number of tachyzoites was calculated via a light microscope. The level of liver lipid peroxidation (LPO) and nitric oxide (NO), toxicity effects on the liver and kidney, and the mRNA expression levels of some pro-inflammatory cytokines such as IL-1β and IFN-γ were determined by quantitative real-time PCR.ResultsDifferent concentrations of ASEO showed a significant (p < 0.001) anti-Toxoplasma activity against T. gondii tachyzoites, and the highest efficacy was observed at the concentration of 150 µg/mL. Fourteen days of pre-treatment of infected mice with ASEO at the doses of 200, 400, and 600 µg/kg/day significantly (p < 0.001) decreased the mean number of tachyzoites and mortality rate by the 6th, 7th, and 8th days after infection, respectively. ASEO at the doses of 200, 400, and 600 µg/kg/day significantly (p < 0.05) improved the increase in the LPO and NO. Pre-treatment of mice with different doses of ASEO provoked a considerable (P < 0.001) downregulation of IL-1β and IFN-γ mRNA gene expression levels, but it had no significant toxicity on the serum levels of some liver and kidney enzymes.ConclusionThe present study demonstrated the considerable prophylactic effects of ASEO that increased the survival rate of mice and reduced the parasite load in them. Our findings also showed that ASEO promotes the innate immune system, pro-inflammatory cytokines, inhibition of hepatic injury, etc. in the mice with acute toxoplasmosis. However, additional investigations are mandatory to clarify the accurate prophylactic and therapeutic anti-Toxoplasma mechanisms of ASEO as well as all its toxicity aspects, especially in clinical settings.

Estimating the Optimal Dexketoprofen Pharmaceutical Formulation with Machine Learning Methods and Statistical Approaches.

ObjectivesOrally disintegrating tablets (ODTs) can be utilized without any drinking water; this feature makes ODTs easy to use and suitable for specific groups of patients. Oral administration of drugs is the most commonly used route, and tablets constitute the most preferable pharmaceutical dosage form. However, the preparation of ODTs is costly and requires long trials, which creates obstacles for dosage trials. The aim of this study was to identify the most appropriate formulation using machine learning (ML) models of ODT dexketoprofen formulations, with the goal of providing a cost-effective and time-reducing solution.MethodsThis research utilized nonlinear regression models, including the k-nearest neighborhood (k-NN), support vector regression (SVR), classification and regression tree (CART), bootstrap aggregating (bagging), random forest (RF), gradient boosting machine (GBM), and extreme gradient boosting (XGBoost) methods, as well as the t-test, to predict the quantity of various components in the dexketoprofen formulation within fixed criteria.ResultsAll the models were developed with Python libraries. The performance of the ML models was evaluated with R 2 values and the root mean square error. Hardness values of 0.99 and 2.88, friability values of 0.92 and 0.02, and disintegration time values of 0.97 and 10.09 using the GBM algorithm gave the best results.ConclusionsIn this study, we developed a computational approach to estimate the optimal pharmaceutical formulation of dexketoprofen. The results were evaluated by an expert, and it was found that they complied with Food and Drug Administration criteria.

Ethnopharmacological Study of Medicinal Plants in Bajwat Wildlife Sanctuary, District Sialkot, Punjab Province of Pakistan.

Bajwat Wildlife Sanctuary is a complex riverine ecosystem and is unique because of the presence of river Chenab, various seasonal streams, lakes, and Head Marala barrage. These ecogeographic conditions provide diverse natural habitats for various plant and animal species to grow uninterrupted and have undocumented ethnopharmacologically important medicinal flora. The present study involves the first-ever extensive investigation to document the ethnopharmacological knowledge on medicinal plants of local healers and inhabitants of the Bajwat Wildlife Sanctuary to treat ailments. The unstructured and semistructured interviews of the local healers and inhabitants were conducted that included 130 individuals. The ethnomedicinal formulations, their method of preparation, mode of administration, parts of the plant used, diseases cured, and their categorization along with species use report (UR) were analyzed. The ethnopharmacological study led to the enlisting of 114 medicinal plant species belonging to 97 genera and distributed among 47 plant families. 2029 URs were collected with 42 general disease categories. Each plant species was reported 18 times to cure various diseases (∼18 UR), while ∼48 URs were collected on each disease category by local informants. Digestive issues (290 URs, ∼14.29%) and skin infections (279 URs, ∼13.75%) were found most commonly among the occupants of the area. The oral administration (69%) of herbal drugs and the preparation of plant extracts (32%) were the most common ethnopharmacological strategies. Inhabitants of the area were well aware of the limited use of poisonous plants. 8 (∼7%) out of the total 114 medicinal plant species were listed in the IUCN Red List of Threatened Species as Least Concern, while Eucalyptus camaldulensis Dehnh. was enlisted as near-threatened. The results of the present investigation show that the occupants of the Bajwat have sound information about the ethnopharmacological consumption of medicinal plants, and some of the novel ethnomedicinal formulations were reported which provide the basic data for further pharmacological research.

Comparison of RPMI 2650 cell layers and excised sheep nasal epithelial tissues in terms of nasal drug delivery and immunocytochemistry properties

Nasal drug administration has been identified as a potential alternative to oral drug administration, especially for systemic delivery of large molecular weight compounds. Major advantages of nasal drug delivery include high vascularity and permeability of the epithelial membranes as well as circumvention of first-pass metabolism. RPMI 2650 cell layers (in vitro cell model) and excised sheep nasal mucosal tissues (ex vivo sheep model) were evaluated with regard to epithelial thickness, selected tight junction protein expression (i.e. claudin-1, F-actin chains, zonula occludin-1), extent of p-glycoprotein (P-gp) related efflux of a model compound (Rhodamine-123, R123) and paracellular permeation of a large molecular weight model compound (FITC-dextran 4400, FD4). The cell model grown under liquid cover conditions (LCC) was thinner (24 ± 4 μm) than the epithelial layer of the sheep model (53 ± 4 μm), whereas the thickness of cell model grown under air liquid interface (ALI) conditions (53 ± 8 μm) compared well with that of the sheep model. Although the location and distribution of tight junction proteins and F-actin differed to some extent between the cell model grown under ALI conditions and the sheep model, the extent of paracellular permeation of FD4 was similar (Papp = 0.48 × 10−6 cm.s−1 and 0.46 × 10−6 cm.s−1, respectively). Furthermore, the bi-directional permeation of R123 yielded the same efflux ratio (ER = 2.33) in both models. The permeation results from this exploratory study indicated similarity in terms of compound permeation between the RPMI 2650 nasal epithelial cell line and the excised sheep nasal epithelial tissue model.

Microencapsulated Isoniazid-Loaded Metal-Organic Frameworks for Pulmonary Administration of Antituberculosis Drugs.

Tuberculosis (TB) is an infectious disease that causes a great number of deaths in the world (1.5 million people per year). This disease is currently treated by administering high doses of various oral anti-TB drugs for prolonged periods (up to 2 years). While this regimen is normally effective when taken as prescribed, many people with TB experience difficulties in complying with their medication schedule. Furthermore, the oral administration of standard anti-TB drugs causes severe side effects and widespread resistances. Recently, we proposed an original platform for pulmonary TB treatment consisting of mannitol microspheres (Ma MS) containing iron (III) trimesate metal–organic framework (MOF) MIL-100 nanoparticles (NPs). In the present work, we loaded this system with the first-line anti-TB drug isoniazid (INH) and evaluated both the viability and safety of the drug vehicle components, as well as the cell internalization of the formulation in alveolar A549 cells. Results show that INH-loaded MOF (INH@MIL-100) NPs were efficiently microencapsulated in Ma MS, which displayed suitable aerodynamic characteristics for pulmonary administration and non-toxicity. MIL-100 and INH@MIL-100 NPs were efficiently internalized by A549 cells, mainly localized in the cytoplasm. In conclusion, the proposed micro-nanosystem is a good candidate for the pulmonary administration of anti-TB drugs.

CHLOROFORM EXTRICATE OF TRIANTHEMA PORTULACASTRUM, WHOLE PLANT: AN ANTI-HYPERLIPIDEMIC IN ATHEROGENIC DIET INDUCED HYPERLIPIDEMIC RATS

Hyperlipidemia is contemplated to be among the considerable risk factor that contributes to the severity as well as incidence of cardiovascular diseases. The Anti hyperlipidemic effect of Chloroform extricate of entire plant Trianthema portulacastrum has been studied in atherogenic diet induced hyperlipidemic rats. Group-I acted as controls (untreated), Group-II acted as atherogenic diet induced controls, standard Hypolipidemic drug (Simvastatin 4mg/kg) used for treating Group-III. The Chloroform Extricate of Trianthema portulacastrum were administered orally at 100mg/kg and 200mg/kg doses for Group IV and V respectively. Serum lipid levels were evaluated after oral administration of standard drug and Chloroform extricate of Trianthema portulacastrum (100mg/kg as well as 200mg/kg) respectively at experimental study’s end. With 200mg/kg of Trianthema portulacastrum Chloroform Extricate treatment, significant reduction in serum lipid parameters like VLDL, LDL, triglycerides, total cholesterol levels and increased HDL level were seen hyperlipidemic rats as compared to control statistically. From these results, it is evident that, Chloroform Extricate of Trianthema portulacastrum entire plant treats hyperlipidemia and improves the liver lipid profile.

Modification of the Release of Poorly Soluble Sulindac with the APTES-Modified SBA-15 Mesoporous Silica

The effectiveness of oral drug administration is related to the solubility of a drug in the gastrointestinal tract and its ability to penetrate the biological membranes. As most new drugs are poorly soluble in water, there is a need to develop novel drug carriers that improve the dissolution rate and increase bioavailability. The aim of this study was to analyze the modification of sulindac release profiles in various pH levels with two APTES ((3-aminopropyl)triethoxysilane)-modified SBA-15 (Santa Barbara Amorphous-15) silicas differing in 3-aminopropyl group content. Furthermore, we investigated the cytotoxicity of the analyzed molecules. The materials were characterized by differential scanning calorimetry, powder X-ray diffraction, scanning and transmission electron microscopy, proton nuclear magnetic resonance and Fourier transformed infrared spectroscopy. Sulindac loaded on the SBA-15 was released in the hydrochloric acidic medium (pH 1.2) and phosphate buffers (pH 5.8, 6.8, and 7.4). The cytotoxicity studies were performed on Caco-2 cell line. The APTES-modified SBA-15 with a lower adsorption capacity towards sulindac released the drug in a less favorable manner. However, both analyzed materials improved the dissolution rate in acidic pH, as compared to crystalline sulindac. Moreover, the SBA-15, both before and after drug adsorption, exhibited insignificant cytotoxicity towards Caco-2 cells. The presented study evidenced that SBA-15 could serve as a non-toxic drug delivery system that enhances the dissolution rate of sulindac and improves its bioavailability.

Intratracheal Administration of Chloroquine-Loaded Niosomes Minimize Systemic Drug Exposure.

Pulmonary administration provides a useful alternative to oral and invasive routes of administration while enhancing and prolonging the accumulation of drugs into the lungs and reducing systemic drug exposure. In this study, chloroquine, as a model drug, was loaded into niosomes for potential pulmonary administration either via dry powder inhalation or intratracheally. Chloroquine-loaded niosomes have been prepared and extensively characterized. Furthermore, drug-loaded niosomes were lyophilized and their flowing properties were evaluated by measuring the angle of repose, Carr’s index, and Hausner ratio. The developed niosomes demonstrated a nanosized (100–150 nm) spherical morphology and chloroquine entrapment efficiency of ca. 24.5%. The FT-IR results indicated the incorporation of chloroquine into the niosomes, whereas in vitro release studies demonstrated an extended-release profile of the drug-loaded niosomes compared to the free drug. Lyophilized niosomes exhibited poor flowability that was not sufficiently improved after the addition of lactose or when cryoprotectants were exploited throughout the lyophilization process. In vivo, intratracheal administration of chloroquine-loaded niosomes in rats resulted in a drug concentration in the blood that was 10-fold lower than the oral administration of the free drug. Biomarkers of kidney and liver functions (i.e., creatinine, urea, AST, and ALT) following pulmonary administration of the drug-loaded nanoparticles were of similar levels to those of the control untreated animals. Hence, the use of a dry powder inhaler for administration of lyophilized niosomes is not recommended, whereas intratracheal administration might provide a promising strategy for pulmonary administration of niosomal dispersions while minimizing systemic drug exposure and adverse reactions.

Formulation, Optimization and Pharmacodynamic Studies of Pioglitazone HCl Solid Lipid Nanoparticles

Pioglitazone HCl is an oral anti-diabetic agent used for the treatment of diabetes mellitus type II. The aim of the present work is to evaluate the pharmacodynamic activity of solid lipid nanoparticles of pioglitazone HCL prepared by using solvent injection technique and to compare with the control and test group. Among all the formulations, F5 was found to possess highest in-vitro drug release within 24 hrs i.e., 95.02±1.26%. The in vivo studies were performed using male albino rats of wistar strain (150-200g). Rats were divided in to five groups (n=6), group-I normal, group-II diabetes control, group-III placebo control, group-IV reference, group-V test group. Diabetes was induced by streptazocin (60 mg/kg) by intraperitonial route. The reference group was treated with marketed tablet of pioglitazone HCL, test groups were treated with SLNs suspended in 0.1% Tween 80 and given to animals through oral gavages. Blood samples were collected by retro-orbital puncture before treatment, and after treatment at time intervals 0, 2, 4, 6, 8, 10, 12 and 24h in anti-coagulated vials. Parameters like glucose, tri glycerides (TG), total cholesterol (TC) and HDL-C were estimated by calorimetric method. Diabetes induced rats showed elevated levels of glucose, TG, TC and reduced HDL. The oral administration of drug loaded SLNs in 0.1% Tween 80 solution showed reduced levels of glucose, TG and elevated levels of HDL-C and slightly reduced levels of TG in 24 h where as the marketed tablet showed reduced levels of glucose, TG and TC up-to 12 h and in 24thh the glucose levels get elevated. Thus the optimized SLNs showed prolonged activity.