Pulmonary Drug Delivery of Peptides and Proteins

From the vial labeled “AE,” aspirin (0.533 g) was placed into a 50 mL Erlenmeyer flask with a boiling stick. Toluene (20 mL) was brought to a boil on a hot plate. The boiling toluene (10 mL) was then added to the aspirin until the solid dissolved completely. After allowing the solution to reach room temperature, the solution was placed in an ice bath for 16 minutes. After the crystals

Pellets are agglomerates of fine powders or granules of bulk drugs and excipients single most important factor responsible for the proliferation of pelletized products is the popularity of controlled release technology in the delivery of drugs. When the pellets containing active ingredient are administered in-vivo in the form of suspensions, capsules, or disintegrating tablets, they offer significant therapeutic advantages over single unit dosage forms, since pellets

Medications that are breathed in (inhaled) can be a good idea if they are to have an effect directly in the lungs. Many asthma medications are available as sprays that are inhaled, for example. Because the lungs

Nanocrystals are made up of drug with only little amount of surfactant (below critical micelle concentration (CMC)) to stabilize formulation [14]. Most of the nanoparticles are made up of large amount of excipients which is not the case with nanocrystals as most of the part is only the drug. Besides lower amount of stabilizers makes toxicity issues associated with nanosuspensions negligible and offers ease of scale-up and better physical stability compared to amorphous form [15, 16]. Different methods are classified as top-down (high pressure homogenization, media milling, and sonication) and bottom-up techniques (nanoprecipitation) for effective production of Nanocrystals [17]. Development of nanocrystal based formulation of risperidone can be advantageous to tackle the problem of poor water solubility. Numerous solidification techniques are used to increase physical stability of nanosuspensions as spray drying, lyophilization and many more based upon the properties of drug and characteristics of final formulation. Amongst all these techniques lyophilization is used predominantly for nanosuspension solidification.

The purpose of this investigation is to find out if the coating on pills makes it harder to dissolve.

Table 1 presents the biodistribution profile (image ROI derived ID/g of tissue) of 68Ga- dicarboxylate dextran in normal rats. The highest uptakes were observed in the heart (blood inside), liver, kidneys and the lungs. Like 68Ga-dextran, a significant uptakes were observed at the bone and cartilage. Compared to the biodistribution of 68Ga-dextran, there is a significant decrease in uptake in the lungs and increased uptake in the kidneys. The high uptake of 68Ga-dextran in the lungs had been attributed to the probable existence of the 68Ga-Dextran precipitate formed in alkaline condition. However, the 68Ga-dicarboxylate dextran was prepared in the mild condition and has high solubility in water. That's why the lungs uptake has sharply decreased.

The experiment was divided into a series of separation phases, a purification phase, and an analysis. Initially, 3.00g of Panacetin was weighed and dichloromethane (DCM) was added to the drug. Sucrose was filtered from this mixture by gravity filtration because it is not soluble in DCM while aspirin and is unknown are. Sodium bicarbonate was then added in order to extract aspirin from the filtrate. The base converted aspirin into its salt, allowing it to move into the aqueous layer of the mixture. The aqueous layers were obtained and hydrochloric acid was added,

Pharmacokinetic analysis suggests that the orally administered nanoemulsions had a higher rate of absorption and the concentration of the drug in the brain and plasma was the highest. Formulation: The drug nanoemulsion was prepared by adding 50% of the drug solution (with dehydrated ethanol) to one ml of safflower oil and it was stirred for the oil drug mixture to distribute homogenously and for all the ethanol to evaporate. Deionized distilled water (contains egg phosphatidylcholine) and deoxycholic acid.(40mg) make up the aqueous phase. Both the phases are heated at 70oc separately. The oil phase was slowly added to the aqueous phase and stirred well. The mixture was then sonicated (21% amplitude and 50%duty cycle). The mixture formed (drug containing nanoemulsion) was then filtered and stored at 4oc.Preparation of aqueous suspension was made using 3H Labeled drug and unlabeled drug in ethanol along with Deionized distilled water (contains egg phosphatidylcholine) and deoxycholic acid. The suspension was sonicated in order to lessen the particle size [2]. An example is Saquinavir (anti-HIV inhibitor) showed enhanced oral absorption and increased concentration of drug in the brain when incorporated in a nanoemulsion

Microspheres formulated using 0.1 M calcium chloride exhibited the highest drug loading at 14%, with 66.5% encapsulation efficiency. Less than 4% and 35% propranolol release occurred from hydrated and dried microspheres, respectively, in 2 hours in simulated gastric fluid (SGF). 90% of the drug load was released in increments of 5 hours and 7 hours from hydrated and dried microspheres, respectively, in simulated intestinal fluid (SIF). Prior incubation of hydrated microspheres in SGF extended the time of release in SIF to 10 hours. Restricted propranolol release in SGF and complete extraction in SIF demonstrate the potential of alginate gel microspheres for oral delivery of

“There are four principal routes through which drugs can be delivered into the body: oral administration, injection, inhalation, and absorption through the skin or membranes” (Levinthal,2012). Consequently, the goal is for drugs to be captivated into the bloodstream. Nevertheless, three ways drugs can be administered into the body would be oral administration, intravenous injection, and inhalation. Conversely, oral administration examples would include pills, marijuana baked in food, methamphetamine, and PCP. Whereas, the advantages would be that taking drugs orally has a slow absorption time frame. And the disadvantages would include no immediate consequence. Nevertheless, intravenous injection examples would include method by needle given to the body in the vein.

This paper discusses some of the different medications used in the treatment of pulmonary hypertension. There are six different articles being used for each the medications, and other basic information pertaining to pulmonary hypertension. The articles discuss studies performed on the drugs to demonstrate their effectiveness on pulmonary hypertension. The articles exhibit important information about how the therapeutic effects of the drugs have different levels of success in varying patients. A few of the most common medications used in the treatment of pulmonary hypertension being discussed in this review are: Vasodilators, High-Dose

The most commonly used water miscible cosolvents are polyethylene glycol 300 and 400, propylene glycol, ethanol, glycerin, dimethylacetamide (DMA), N-Methyl-2-pyrrolidone (NMP), dimethylsulfoxide. Yalkowsky, S.H. et al studied effect of cosolvents on solubility of cyclosporin A in presence of propylene glycol, poly ethylene glycol, tetra hydro furfuryl alcohol, glycerine, ethanol [31]. Poly ethylene glycol 400, Propylene glycol, Ethanol has been used as co solvent for increasing solubility of Ibuprofen [35]. Poly ethylene glycol 400, water can be used as co solvent to enhance the solubility of Valdecoxib [36]. Solubility of carbendazim can be increased by using cosolvents poly ethylene glycol 400, propylene glycol, glycerine, and ethanol

Oral delivery of anti-cancer drugs is a greater advancement in chemotherapy, which offers “Treatment at Home” a dream of cancer patients that improves patient compliance with reduced adverse effects. Cancer chemotherapy, mostly involves parenteral administration of anti-cancer drugs either by intravenous infusion or bolus injection, which is associated with serious side effects due to high plasma drug levels above maximum tolerable concentration (MTC) and is also less effective route due to the short exposure time of anti-cancer drugs to cancerous tissue by rapid excretion of the drug from systemic circulation [1]. In contrast, oral chemotherapy improves therapeutic efficiency by maintaining reasonable plasma drug levels, prolonged exposure time of anti-cancer drugs and avoids side effects by maintaining the drug concentration below MTC by moderate prolonged absorption from the gastrointestinal tract into systemic circulation [2]. Docetaxel is a highly effective second-generation taxane anticancer drug used in the treatment of breast cancer, ovarian cancer, non-small cell lung cancer and other tumors [3-6]. However, oral delivery of docetaxel has negligible oral bioavailability ( 99.9%). Accurately weighed sample (4 mg) was placed in a flat bottomed standard aluminium pan and scanned at a scanning speed of 10°C/min from 30○C to 300○C under a nitrogen gas flow of 80 mL/min.

For example, diverse structures can be gained upon dehydration of the hydrocolloid making. These structures can be customized by the ventilation conditions and formulation making. (Katzung 2004 160-240)Structural characteristics for example porosity might influence the diffusion rate of liquid into the making and thus adjust the release prototype of the drug. Additionally, hydrocolloid-formulation grounding procedures are usually fairly easy and the cost of such materials is small. Diltiazem hydrochloride is a calcium antagonist used to moderate systemic hypertension. Antiarrhythmic effects of the drug control the ventricular response to atrial fibrillation and flutter. This mix is also used for the handling of steady and unbalanced angina pectoris. Although most of the administered drug dose is absorbed (90%), its bioavailability only reaches 3065% because of a high first-pass effect, mainly in the liver and the gastrointestinal tract. (Zohar et al 2004 249-58)Diltiazem hydrochloride has a short plasma half life of 34 h1 and should be taken three to four times a day. Consequently, controlled/sustained-release mixtures for diltiazem hydrochloride are desirable. The objectives of this study were to formulate and characterize dried carriers based on alginate, agarose, and gellan that contain fillers (talc, kaolin, calcium carbonate, potato starch, and corn starch) and diltiazem hydrochloride. (Panchgnula and Thomas 2000 131-50) These fillers are sold as powders and

There are many new ways that are currently being used to improve the oral bioavailability of protein therapeutics. One way is to create microspheres of the product. This can increase bioavailability of the oral route. There are some drugs that are have microsphere technology but no FDA approved oral microspheres peptides. There are a few drug products that have been microencapsulated, Micro-K, Raloxifene Hydrochloride, and insulin. The Micro-K is an FDA approved drug product and it provides an extended release oral dosage form that some patients prefer. It releases potassium slowly in the GI tract like other extended release forms.