Recent advances in drug delivery and formulation最新文献

The pulmonary drug delivery system is a minimally invasive method of administering drugs with systemic and localised activity. Since 4000 BC, inhalation therapy has been known to the Indians. The most effective and suitable pulmonary drug delivery methods have been used for controlling diseases like asthma, chronic obstructive pulmonary disorder (COPD), TB(Tuberculosis), lung cancer, cystic fibrosis, and pulmonary hypertension. Examples of pulmonary medication delivery devices- Metered dose inhalers (MDIs), nebulizers, and dry powder inhalers (DPIs) in the latest patent 2022 that have undergone numerous advancements over the years have been focused on in this article. Some promising patented design advancements of nebulizers are humidifier breathing circuits to control liquid contamination, technologically advanced nebulizers to increase pressure detection and nebulizer disinfection system to decrease or eliminate contagions in expelled air are highlighted in this article. Some noticed formulation-related advancements for inhalational dry powder patented in the year 2022, are mentioned in this article. Development of heat-stable dry powder to solve instability of inhaled protein and peptide powder at high temperatures. The inability of dry powder inhaler devices to administer low doses is solved by designing an affordable and side effects-free inhaler. pMDI manufacturing process is simplified by manufacturing tablets to be administered in pMDI. An aid is developed to lessen the activation force and keep the dose count within budget. The patented advancement in the pulmonary drug delivery system can help in the improvement of patient compliance and drug delivery efficacy.

Over the last few decades, hot melt extrusion (HME) has found extensive adaptability and utility as a viable drug delivery option in the pharmaceutical industry. HME has already been validated as a robust, novel technique mainly used for the correction of solubility and bioavailability of poorly soluble drugs. In line with the scope of the current issue, this review appraises the value of HME as a means of solubility enhancement of BCS class II drugs and presents an influential tool for the manufacturing or production of drugs or chemicals. The drug development process can be shortened with the use of hot melt extrusion technology, and the application of this process to analytical technology can ease the manufacturing process. This review focuses on the tooling, utility, and manufacturing aspects associated with hot melt extrusion technology.

Kojic acid (KA), a fungal secondary metabolite, is commonly used in the cosmetic industry as a skin-whitening agent because of its ability to inhibit tyrosinase, the enzyme involved in melanin production. However, KA has shown poor depigmenting effects and becomes unstable after prolonged storage. Its use in cosmetics products has also been restricted due to its hydrophilic nature. To overcome these limitations, the structure of KA can be altered to form KA derivatives, such as KA ester (KAE), with improved chemical and biological properties. For instance, multiple studies have shown that KAE is more effective at inhibiting tyrosinase, is less toxic and more stable than KA, thus making it more beneficial. Aside from structural modification, nanotechnology applications such as nanoemulsion, and others have shown the ability to strengthen the efficacy of both KA and KAE by increasing skin permeability and delivering the drug more precisely to the targeted site with better controlled release rate. Therefore, the aim of this review article is to discuss the importance of modifying KA's chemical structure as well as the role of nanoemulsion, solid lipid nanoparticles (SLN), nanostructured lipid carrier (NLC), liposomes and ethosomes in improving topical delivery of KA and KAE for cosmetic and pharmaceutical applications.

Background: This study aims to formulate and characterize sorafenib-loaded resealed erythrocytes (SoRE) and investigate their anticancer activity in a rat model of hepatocellular carcinoma.

Methods: SoRE were prepared by hypotonic dialysis of red blood cells obtained from Wistar rats using a range of drug-containing dialysis mediums (2-10 mg/ml) and osmosis time (30-240 mins). Optimized SoRE (8 mg/mL and 240 mins) were characterized for size, morphology, stability, entrapment efficiency, in vitro release profiles, and in vivo efficacy evaluations. For efficacy studies, optimized SoRE were intravenously administered to Wistar rats having hepatocellular lesions induced by aflatoxin B and monitored for in vivo antineoplastic activity.

Results: The amount of sorafenib entrapped was directly proportional to the drug concentration in the dialysis medium and duration of osmosis; highest for 10 mg/mL and 240 minutes and lowest for 2 mg/mL and 30 minutes, respectively. Optimized SoRE were biconcave with a size of 112.7 nm and zeta potential of -11.95 ± 2.25 mV. Osmotic and turbulence fragility were comparable with native erythrocytes.

Conclusion: Drug release follows the first-order pattern. In vivo investigations reveal better anticancer activity of SoRE formulation compared to sorafenib standard preparation. Resealed erythrocytes loaded with sorafenib displayed first-order in vitro release and promising anticancer activity in a rat model of hepatocellular carcinoma.

The majority of drugs taken orally have limited aqueous solubility and dissolution rate. Cyclodextrin (CD) and its derivatives are used as pharmaceutical adjuvants, contributing to the development of safe and high bioavailability formulations. CDs have a unique structure with a variety of physicochemical features that aid pharmaceutical scientists in solving drug delivery issues for poorly water-soluble drugs (PWS). This article covers information about cyclodextrin and its various derivatives, its different manufacturing process, physicochemical properties, advantages, and recent advancements. There are various advantages of CD-based inclusion complexes, such as enhancement of solubility, bioavailability, and stability and reduction of irritation caused by the drug. Moreover, they are used as odor and taste enhancers and also prevent incompatibility by physically isolating the incompatible drug components in drug formulation. CD and its derivatives are extensively employed as solubilizers in the manufacturing of parenteral and oral dosage forms. Inclusion complexes formed by CDs with appropriately sized guest molecules improve drug water solubility, physical-chemical stability, and bioavailability. Simultaneously CDs prevent the drugs from degradation like oxidation, hydrolysis, and photodegradation and extend the shelf life of the drug. The manuscript also highlights patents and exclusive branded formulations of modified CDs. It also discusses the different examples of chemically modified CDs, i.e., captisol, sulfobutyl ether-β-CD, hydroxy propyl betadex, randomly methylated β-CD, methyl β-CD, and hydoxy propyl γ-CD, all are used in the various dosage forms.

Objective: This study aimed to evaluate Cola acuminata gum (CAG) for the formulation of mucoadhesive sustained-release matrix tablets of diclofenac sodium.

Methods: Different batches of granules containing CAG and 100 mg of DS in ratios 0.5:1, 1:1, 2:1, and 3:1 were prepared, compressed into tablets, and evaluated for mucoadhesive strength, swelling index, and drug release in SGF (pH 1.2) and SIF (pH 7.4).

Results: Swelling indices and mucoadhesive strengths of the tablets were pH-dependent. Swelling indices of 56 ± 2.03 to 121 ± 2.19% and mucoadhesive strengths of 7.25 ± 1.45 to 15.43 ± 2.71 g/cm² obtained at pH 7.4 were significantly higher (p<0.05) than swelling indices of 25 ± 2.43 to 47 ± 3.15% and mucoadhesive strengths of 5.52 ± 0.76 to 9.22 ± 1.95 g/cm² obtained at pH 1.2. The percentage release of DS from the matrix tablets at pH 1.2 after 2 h (T₂h) was insignificant. However, the percentage of drug release at pH 7.4 was significant for all the batches and dependent on the CAG concentration. The drug release was in the order of batches containing 3 g (80.44 ± 7.75) < 2 g (86.35 ± 5.65) < 1 g (90.08 ± 6.14) < 0.5 g (99.70 ± 3.90). The time for maximum drug release was 7 h (T_7h) for CAG containing 0.5 g and 10 h (T_10h) for other batches.

Conclusion: This study showed that CAG could be useful for mucoadhesive sustained drug delivery.

Background: The current research focused on the improvement of drug entrapment efficiency and release study of hydrophilic drug through polymer complextation.

Objective: Ionotropic gelation technique was utilised for the preparation of Polyelectrolyte complex microbeads of Vildagliptin using Sodium alginate and Eudragit RL100 and their performance was optimized by Central composite design.

Methods: Fourier Transform Infrared Spectroscopy, Scanning Electron Microscope, Differential Scanning Calorimetry, particle size, Drug Entrapment Efficiency, X-ray diffraction and in vitro drug release at 10hr were chosen for evaluating formulated microbeads. The impact of independent variables like concentration of sodium alginate and eudragit RL100 was examined over dependent responses.

Results: The interpretation of XRD, SEM, DSC, and FTIR affirmed no drug excipients interference and confirmed formation of polyelectrolyte complex microbeads. For complex microbeads, the maximum and minimum drug release after 10 hours was obtained as 96.23.5% and 89.45%, respectively. The 32 central composite design was further used to obtain response surface graph and the values for the particle size, DEE and Drug release were retained as 0.197, 76.30 % and 92.15%, respectively for the optimize batch.

Conclusion: The result suggested the combination of two polymers (Sodium alginate and Eudragit RL100) were suitable for improving the entrapment efficiency of hydrophilic drug (Vildagliptin). The central composite design (CCD) technique is an effective tool for obtaining optimal drug delivery systems of Vildagliptin polyelectrolyte complex microbeads.

Deep eutectic solvents (DESs) containing bioactive have been explored as potential choices for therapeutic efficiency enhancement. DESs are regarded as superior compared to established solvents owing to accessibility, storage conditions, synthesis, and low cost. As such, intensive research has taken place in different disciplines, especially nutraceuticals, foods and pharmaceuticals. The applications of DESs, especially in nutraceuticals and pharmaceutical delivery, have shown great promise. Despite these different successes, the safety issues of these DESs need to be properly identified. A safe mixture of DESs must be developed to take its broad range of advantages to the nutraceutical industry, and, therefore, its nutraceutical applications can only be introduced if DESs are known to have profiles of negligible or minimal toxicity. This review emphasizes the fundamental aspects needed to have a better understanding of DESs. It covers the current prospects of DES, including types, properties, formulation components and characterization methods. The several characterization methods, viz., pH, density, refractive index, viscosity, surface tension, solubility, polarized optical microscopy, x-ray diffraction studies, Fourier transforms infrared spectroscopy, and nuclear magnetic resonance spectroscopy are also mentioned. Further, the promising applications of DESs in different nutraceutical and pharmaceutical domains are highlighted.