Nanoparticle formulation by Büchi B-90 Nano Spray Dryer for oral mucoadhesion

Abstract

Diabetes is considered one of the main threats to global public health in this era. It is increasing rapidly in every part of the world; the prevalence of the disease will grow to the point where 366 million people will be affected by 2030. The prevalence of diabetes mellitus (DM) in the Saudi population is high, and the majority of patients suffer from type 2 DM. Marketed oral antidiabetic drugs have indicated poor tolerability during chronic treatments, and this contributes to the moderately large proportion of type 2 DM patients that remain inadequately managed. Vildagliptin nanospheres were prepared with aminated gelatin using a spray-drying method; narrow particle-size distribution was seen at 445 nm. The angle of repose was found to be θ <33.5°. The nanospheres appeared to be spherical with a smooth surface. The drug content and percentage yield of the nanospheres were found to be 76.2%±4.6% and 83%±2%, respectively. The nanosphere-swell profile was found to be 165%±7%. The pure drug was 100% dissolved in 30 minutes, and the nanosphere formulation took 12 hours to dissolve (97.5%±2%), and followed a Korsmeyer–Peppas kinetic model with an R2 of 0.9838. The wash-off test of nanospheres found that they exhibited an excellent mucoadhesive property at 86.7% for 8 hours. The stability-study data showed no changes in the physicochemical properties of the nanospheres, and suggested that the nanospheres be stored below room temperature. The amount of vildagliptin retained was 1.6% within 3 hours, and in comparison with the gelatin vildagliptin nanoparticles formulation, the percentage that was retained was much higher (98.2% in 12 hours).

HPMC- and PLGA-Based Nanoparticles for the Mucoadhesive Delivery of Sitagliptin: Optimization and In Vivo Evaluation in Rats

“…The filtered solution was used to avoid any nozzle blockage while spraying. The spray-dried particles were scraped out manually from the particle collecting chamber using a rubber scraper [14].…”

“…Moreover, the final product may become contaminated by residual solvent from drug-excipient interaction, packaging, or in the accelerated decomposition of the formulation. Manufacturers are responsible for minimizing the organic solvent within the specified limits due to toxicological reasons and due to the lack of therapeutic benefits [14]. The development of a spray-drying technology is not new as far as the drug manufacturing industries are concerned.…”

Novel Preparation and Effective Delivery of Mucoadeshive Nanoparticles Containing Anti-diabetic Drug

“…14,15 In order to sustain therapeutic effects of a drug at site of absorption, recent efforts have focused on development of mucoadhesive delivery systems using nanoparticles. 16,17 Such systems make use of a mixture of the mucoadhesive polymer to form mucoadhesive devices which adhere to mucous intestinal lining releasing drug load slowly. 16 The mucoadhesive drug delivery systems are advantageous over the other existing delivery systems in that not only they target and localise dosage form specifically, but also result in higher drug flux at the absorption site in the Gastrointestinal tract (GIT), stabilise drug fluctuations in the plasma as well as reduce side effects.…”

Influences of copolymers (Copovidone, Eudragit RL PO and Kollicoat MAE 30 DP) on stability and bioactivity of spray-dried and freeze-dried lysozyme

“…The most frequently used method to produce solid state protein formulations with a considerable stability is spray drying (see for example, (2,4,5) and freeze drying (see for example, (6-8). Another method used to stabilise proteins is by adding wide variety of excipients to stabilise proteins (see for example, (2,9,10).…”