Bioavailability

Black pepper, also designated as ‘King of spices’ a characteristic familiar global spice related to the Piperaceae family and generally used in culinary and medicinal preparations. Its pungency is due to piperine, volatile elements and essential oil. Piperine is an amide alkaloid, effective bioactive present in piper species of black and long peppers; and reveals several potential therapeutic actions to intervene different disease conditions whereas functional group responses at active site liable to act as a xenobiotic bio-enhancer and an effective CNS stimulant. However, piperine is slightly soluble in water, limiting its pharmacological activities and biomedical services. It is solid crystalline nature, mild basic, initially tasteless while, a burning after taste. Therefore, this bioactive natural substance should be considered in the arenas of rational drug design and development of formulations. Recent developments in drug delivery system have to overcome its limitations, including poor bioavailability and blood–brain barrier permeability.  Chaperons like phytosomes are encouraging tools to alter oral absorption of piperine. The study highlights the prepared and correctly recognized piperine-phospholipid complex (PPC) in terms of FT-IR (Fourier Transform Infra-red spectroscopy), DSC (differential scanning calorimetry), XRPD (X-ray powder diffractometry), and SEM (scanning electron microscopy). The PPC was found to be fine and loose, airy, light, rough surface with improved water solubility and bioavailability.

Nasal drug delivery system offers way of drug delivery of both topical and systemic therapies. The high permeability, high vasculature and low enzymatic environment of nasal cavity are well suitable for systemic delivery of drug molecules via nose. The despite of all the advantages of nasal drug delivery, the bioavailability of nasally administered products, especially for protein and peptide molecules, is affected by many barriers such as physiological barriers, physicochemical barriers, and formulation barriers. This review will focus on the various bioavailability barriers in nasal drug delivery and the strategies to improve the bioavailability of nasal dosage form

Oral route has been considered as most convenient route but restricted to only hydrophilic compounds having GI stability and greater dissolution. The delivery of lipophilic compounds has been area of interest since most of the drugs under discovery shows limited bioavailability. Self-emulsifying delivery systems (SMEDDS) has drawn a greater attention in the formulation of poorly soluble compounds where increase in the absorption and permeation of the drug has observed. The self-emulsification which occurs in the case of SMEDDS has shown a potential advantage over conventional emulsion due to the fine globules formed upon dilution. The recent trends such as dry emulsion, s-SMEDDS, SNEDDS thoroughly investigated. This article, attempts to present the overview of the SMEDDS along with its formulation, application and characterization.

Phytoconstituents, in modern time phytosomes are being increase the level of natural remedies. It is recently introduced system to have used as a novel drug delivery. However nowadays it has been developed into the most well-turned and self assembled system to raise the oral bioavailability of phyto-drugs. That generally recognized as phytosomes. Phytoconstituents have a benignant moderation between hydrophilic and lipophilic in nature molecules which is helps in breakdown of gastro-intestinal sap to pass the lipid rich bio-membrane of cells. It can just be achieved as a result of phytosomes technique. But the delivery of herbal drugs is turn into the challenges owing to reduced aqueous dissolubility, poor permeations and foremost metabolite rate. Therefore, phytosome works as linkage for retain the efficiency toward develop the incorporation of numerous well-liked herbal drugs. E.g. - Ginkgo biloba, grape seeds, green tea etc. it can merely be evolved for a variety of remedial use.

The present study aimed at improvement of solubility and bioavailability of Lercanidipine HCl using self-nanoemulsifying drug delivery systems (SNEDDS). The extent of self-emulsification was checked with various oils with suitable surfactants and co-surfactants. The final optimized formulation contained Caproyl 90, Tween 80 and Labrosol as oil, surfactant and co-surfactant respectively. Based on Lercanidipine solubility analysis, ternary phase diagrams were constructed for optimizing the system. The formulations were evaluated for solubility, droplet size determination, zeta potential and stability studies. The droplet size was found to be 5.1 nm & Z-Average of 14.6 nm. The zeta potential of the optimized formulation (F16) was found to be -19.7 mV. In vitro drug release from SNEDDS was significantly higher than pure drug. From in vivo bioavailability studies the optimized formulation was exhibited a significantly greater Cmax (56.2±0.04ng/ml) than the pure drug suspension (35.1±0.03ng/ml). AUC0-∞ for SNEDDS formulation was higher (190.5±2.04 ng.h/ml) than the pure drug suspension 145.7±2.02ng.h/ml. Statistically, AUC0-t of the SNEDDS formulation was significantly higher (p<0.05) as compared to pure drug suspension formulation. The study demonstrated that SNEDDS was a promising strategy to enhance the solubility and oral bioavailability of Lercanidipine.

Naringenin is a flavonoid which has been used for its wide pharmacological action from ancient years including as antidiabetic agent. Naringenin is a lipophilic drug (BCS-II) and have low water solubility (1 in 1000), bioavailability (<25%) and have short half-life (t1/2 =1.3 -2.2h). Nanocrystals is an approach to increase the therapeutic performance of poorly water soluble drugs. The purpose of the present study was to prepare nanocrystalss of naringenin to improve bioavailability and increase therapeutic efficacy. Nanocrystalss of naringenin were prepared by antisolvent precipitation method. The stabilizers used to improve aggregation and increase the solubility. Nanocrystals were characterized for particle size, morphology, release profile and thermal analysis.

Melt granulation has gathered increasing interest in the pharmaceutical industry for the concept of utilizing a molten liquid as a binder. Melt granulation process is currently applied in the pharmaceuticals for the manufacture of variety of dosage forms and formulation such as immediate release and sustained release pellets, granules and tablets. This technique has been used for improving bioavailability of poorly water soluble drugs. The review article gives updates about the latest developments in technology behind use of melt granulation process. Article deals with in depth basic information about granule growth mechanisms during melt granulation. The article also provides an insight to Equipments and factors influencing the melt granulation process & its applications to improve the dosage form characteristics which are utilized for industrial production.

The purpose of this research work was to formulate fast dissolving film of cefpodoxime proxetil for oral delivery in order to improve oral bioavailability of drug with poor solubility. Cefpodoxime proxetil (CP) is the drug candidate belonging to BCS class IV with poor solubility and poor permeability is and limited oral bioavailability, an orally administered, extended spectrum, semi-synthetic β- lactum antibiotic of cephalosporin class. To improve oral bioavailability, cefpodoxime proxetil nanosuspension was prepared using solvent-antisolvent precipitation technique. Nanosuspension was characterized on the basis of drug concentration in organic phase, temperature, solvent-antisolvent ratio and the time period of stirring on the particle size systematically. Particle size and zeta potential of nanosuspension was observed at 755.6nm and −22.6mV, respectively. Solvent casting method be used in the formation of film, utilizing HPMC E50 as film former, PEG 400 as plasticizer and tween 80 as surfactant. The optimized fast dissolving film formulation F1 showed uniformity of weight (0.091mg), folding endurance (149) drug content uniformity (99.5%), surface pH (6.8) disintegration time (32 seconds in 6.8 PB) and in- vitro drug release 94.2% in 7 min. So, it is concluded from comparison studies between fast dissolving film (FDF) containing pure drug and nanosuspension, fast dissolving film containing cefpodoxime proxetil nanosuspension gives faster and high drug release.

Among the different routes of drug administration the oral route is most successful and popular. Dosage forms with a prolonged gastric residence and controlled drug delivery are called as Gastroretentive Drug Delivery System. Thus, these dosage forms significantly extend the period of time over which the drugs may be released in comparison to other Controlled Release Drug Delivery System. Different objectives that are to be achieved during development of gastro retentive drug delivery system are as it should increase bioavailability of drug, increase residence time of dosage form in stomach, achieve greater patient compliance by reducing frequency of dosing, better safety profile, achieve the improved economy of dosage form.This review covers major aspects of stomach anatomy and physiology, factors, rational, objectives, approaches, evaluation of gastroretentive drug delivery system.

Bioavailability may be considered as one aspect of drug product quality that links the in-vivo performance of the drug product used in clinical trials with studies demonstrating evidence of safety and efficacy. In the present study, the bioavailability was performed for the qualitative evaluation of the L-lysine produced by modified Corynebacterium glutamicum. Thirty 3-week-old male Sprague-Dawley rats weighing 45-55 g were used. The animals were divided into three groups. The first group was kept on a protein free basal diet which was supplemented with the biotechnologically modified L-lysine from Corynebacterium glutamicum. The second group comprised of animals which were fed the same basal diet but supplemented with a marketed preparation of L-lysine. The third group was kept on a regular protein diet which served as a control. The animals were fed ad libitum for 13 days, during which weight gain and food consumption were recorded and food conversion efficiency (FCE; weight gained/weight food eaten) was calculated. Ratios of means were calculated using the (least-square means)LSM for untransformed and ln-transformed FCE. The bioavailability was estimated by measuring the pharmacological activity (weight gained) and compared with that of the marketed preparations of L-lysine under similar conditions. For the study reference and test samples,-s the 95% confidence interval fell within the range of 97.72 and 103.61, which was the indication of bio similarity for biological activity of both the samples.