Design and Development of Self-Microemulsifying Drug Delivery Systems (Smedds) of Telmisartan for Enhancement of in Vitro Dissolution and Oral Bioavailability in Rabbit

Abstract

Objective: The main purpose of this investigation was to prepare self-microemulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of a poorly water soluble drug telmisartan (TLS), a BCS class II drug by improving its dissolution rate. Methods: Self-Emulsifying Drug Delivery Systems (SEDDS) of TLS were formulated using cinnamon essential oil as the oil phase, Gelucire 44/14 as the surfactant and Transcutol HP as co-surfactant. Drug-excipient interactions were studied by FTIR spectroscopy. The formulations were evaluated for its self-emulsifying ability, clarity, and stability of the aqueous dispersion after 48 h and the phase diagram was constructed to optimize the system. Selected formulations were characterized in terms of droplet size distribution, zeta potential, cloud point and were subjected to in vitro drug release studies. The bioavailability of optimized formulation was assessed in New Zealand white rabbits.Results: By considering smaller droplet size, higher zeta potential and faster rate of drug release the formulation TF9 was chosen as optimized SMEDDS formulations. TF9 was robust to different pH media and dilution volumes, remained stable after three cooling-heating cycles and after stored at 4 °C and 25 °C for 3 mo without showing a significant change in droplet size. The pharmacokinetic study in rabbits showed SMEDDS have significantly increased the Cmax and area under the curve (AUC) of TLS compared to suspension (P<0.05).Conclusion: SMEDDS can be an effective oral dosage form for enhancing aqueous solubility and improving oral bioavailability of poorly water soluble drugs.

Use of Simplex Lattice Design in Development of Oral Self-Nanoemulsifying Drug Delivery System Containing Rosuvastatin Calcium

“…Rosuvastatin calcium is a lipid-lowering drug was an attractive candidate for the current study because it is a lipophilic compound with partition coefficient; log P = 4.81 and low aqueous solubility (0.00936 mg/ml). The current rosuvastatin calcium commercially marketed dosage forms is tablets and these show low (about 20%) and erratic oral bioavailability [3,4]. The aim of the present study is bioavailability enhancement of rosuvastatin calcium and find the optimum formula of rosuvastatin calcium SNEDDS followed by characterization.…”

Formulation and Evaluation of Solid Self Micro Emulsifying Dispersible Tablet of Piroxicam

“…Later, surfactants like Cremophor RH 40, OP-10, and Tween 80 were combined amidst all oils. The marked surfactants, which revealed the poor capacity to form a microemulsion, were graded as D and E and which showed the good capacity of forming microemulsion were graded A and B [32]. However, Cremophor R H-40 produced fine microemulsion among all, as most of it got visual class as B.…”

Self-Micro Emulsifying Drug Delivery System of Ursolic Acid: Formulation Development, Characterization, Pharmacokinetic and Pharmacodynamic Studies for Diabetic Complications

“…After that, the mixture was cyclo mixed for 20 min to produce a translucent uniform mixture. The formulations oil, surfactant, and co-surfactant ratios were altered [15]. The various compositions are listed in table 2.…”