During the twenty-first century, drug discovery is expanding rapidly and a large number of chemical moieties are recognized. Many of them are poorly soluble and hence related biopharmaceutical constraints are to be addressed systematically. Among novel approaches to resolving biopharmaceutical issues, micro- and nano-emulsified systems serve as the best strategy for delivering both hydrophobic and hydrophilic drugs owing to their greater solubilization and transportation capabilities. Of late, the unique physical and biopharmaceutical properties of these liquid isotropic homogenous systems have gained substantive research importance. In addition nano/micro lipid systems share structural and functional similarity with that of the physiological lipids which offer better tolerance ability in the body. In this context, this article provides information on the historical emergence of particulate emulsified systems, importance and rationale of selection of carriers. It also encompasses the physicochemical principles that are responsible for the elevation of therapeutic outcomes of delivery systems. Detailed and schematic absorption of these drug delivery systems is explained here. Gastro-intestinal biochemistry necessary in the understanding of digestion process, lipolytic products formed, micellar structures, enzymes, transporters, mechanism of cell uptake involved after subsequent oral absorption are also emphasized. In addition, this article also explains disposition and pharmacokinetic properties of emulsified systems with real-time therapeutic research outcomes. The influence of biochemical compositions and biopharmaceutical principles on absorption and disposition patterns of ME/NEs was described in the article for the interest of readers and young researchers.
The goal of this research is to develop captopril mouth dissolving films and evaluate the impact of various formulation factors on the physical and mechanical properties of the films, as well as drug release behaviour. In different grades, hydroxypropyl methyl cellulose (HPMC E15 and K4M) was employed as the film forming polymer. Formulation disintegration times were determined to be in the range of (52 2.5 to 125.6 2.02 s). Formula F2 had the fastest disintegration time in vitro (52 2.5 s) and was determined to be acceptable for film production with ideal physicochemical qualities, faster disintegration, and optimal in vitro release. It may be concluded that the solvent casting approach can be used to make captopril mouth dissolving films with a higher dissolution rate and greater patient compliance.
Diklofenak sınırlı çözünürlük, düşük biyoabsorpsiyon ve gastrik toksisite gösterir. Çalışmanın amacı, yukarıdaki kısıtlamaları ele almak ve RA'nın kronoterapisi için çok birimli bir formülasyon tasarlamaktır. Gereç ve Yöntemler: DC, SSG ve GG ile katı dispersiyonları hazırlandı. Aynı boyutlu (∼400 µm) nonpareil çekirdekler, hemen salım yapan pelletler (DMP-1 ve DMP-2) ve kontrollü salımlı pelletler (DMP-3 ve DMP-4) üretmek için katı dispersiyonlarla kaplandı. Elde edilen kontrollü salım pelletleri, pulsatil salım pelletleri (DMPP) elde etmek için metakrilat polimerleri ile daha da katmanlı hale getirildi. DMPP için çözünürlük, FTIR, DSC, mikrometrik, SEM, etkin madde içeriği, etkin madde salımı, farmakokinetik ve stabilite çalışmaları yapıldı. Bulgular: DC'nin çözünürlüğü, katı dispersiyonlardaki hidrofilik taşıyıcıların varlığına bağlı olarak 164 kat arttı. FTIR spektrumunda ve termogramlarda kimyasal ve fiziksel etkileşimler gözlemlenmedi. Akışkanlaştıran yataklı işlemci, 19.5 dereceden daha az bir akış açısı ve %95.18 ile %98.87 arasında DC içeriği olan yüksek kaliteli, yuvarlak ve düzenli pelletlerin üretimini kolaylaştırdı. Maksimum etkin madde 12 saat sonunda DMPP'den salındı. Objectives: Diclofenac exhibits limited solubility, low bioabsorption and gastric toxicity. The objective of the study was to address the above limitations and to design a multi-particulate formulation for the chronotherapy of RA. Materials and Methods: Solid dispersions of DC with SSG and GG were prepared. Uniform-sized (∼400 µm) non-pareil seeds were coated with solid dispersions to produce immediate-release pellets (DMP-1 and DMP-2) and controlled-release pellets (DMP-3 and DMP-4). The resultant controlled-release pellets were further layered with methacrylate polymers to obtain pulsatile-release pellets (DMPP). Solubility, FTIR, DSC, micrometrics, SEM, drug content, drug release, pharmacokinetics, and stability studies were performed for DMPP. Results: The solubility of DC was improved by 164-folds due to the presence of hydrophilic carriers in the solid dispersions. No chemical and physical interactions were noticed in FTIR spectra and also in thermograms. A fluidized bed processor facilitated the production of high-quality, circular, and regular pellets with an angle of repose less than 19.5 degrees and DC content between 95.18% and 98.87%. The maximum drug was released from DMPP at the end of 12 hours. DMP-1 and DMP-2 pellets had 2 hr of drug release and pulsatile, controlled-release pellets had a 6 hr lag phase followed by 12 hr controlled release. Both DMP-1 and DMP-2-immediate showed first-order release followed by Hixson-Crowell kinetics, whereas DMPP pellets followed zero-order release with Higuchi's kinetics. The maximum concentration of DC in plasma was 400.8 ng/mL at 5 hr for DMP-2 and 381.1 ng/mL at 14 hr for DMPP-5. The solubility of DC was increased with the application of solid dispersion and in turn increased the pharmacokinetics. The pellets were plausibly stable over a period of 90 days. Conclusion: Thus, multi-p...
Chronopharmacokinetics of BD were achieved with the help of Eudragit coatings on pellets. The BMP and BMPP formulations were found to be reasonably stable over a period of time. Thus, optimal chronopharmacokinetics of BD was achieved successfully by multiparticulate pulsatile technology.
The present research was focused to prepare the formulation containing combination of Metformin and Curcumin to control diabetes-induced Alzheimer’s in elderly population with the utilization of Poloxamer P188 (8%), a thermoreversible gelling polymer, and mucoadhesive polymers such as Carbopol 940, Sodium alginate and HPMC K100 in varying concentrations (0.5%, 1%, 1.5% and 2% respectively) to improve the absorption of drugs by increasing the contact time with nasal mucosa. The in situ gel was prepared by cold method and administered via nasal route to deliver the drug directly to CNS by bypassing BBB and to improve patient compliance, nasal bioavailability of drugs by cumulative its nasal retention time in nasal mucosa. Total 12 nasal in situ gels were prepared and evaluated for in vitro studies and ex vivo drug diffusion studies (goat nasal mucosa) and results were found to be satisfactory. Moreover, histopathological studies revealed that the preparation was safe to be used on nasal mucosa of goat. The prepared nasal in situ gel is an effective alternative to conventional method and can be used to treat diabetes-induced Alzheimer’s disease.
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