Sabna Kotta

Potentials and challenges in self-nanoemulsifying drug delivery systems

Introduction: A significant number of new chemical entities (almost 40%), that are outcome of contemporary drug discovery programs, have a potential therapeutic promise for patient, as they are highly potent but poorly water soluble resulting in reduced oral bioavailability. Self-nanoemulsifying drug delivery systems (SNEDDS) have emerged as a vital strategy to formulate these poorly soluble compounds for bioavailability enhancement. Areas covered: The review gives an insight about potential of SNEDDS with regards to oral drug delivery. The effect of various key constituents on formulation of SNEDDS and their applications in oral drug delivery is also discussed. Various aspects of formulation, characterization and biopharmaceutical aspects of SNEDDS are also been explored. The choice and selection of excipients for development of SNEDDS is also discussed. Expert opinion: The ability of SNEDDS to present the drug in single unit dosage form either as soft or hard gelatin capsule with enhanced solubility maintaining the uniformity of dose is unique. With the ease of large-scale production, high drug-loading capacity, improvement in release behavior of poorly water-soluble drugs and improvement of oral bioavailability, SNEDDS have emerged as preferable system for the formulation of drug compounds with bioavailability problems due to poor aqueous solubility.

Self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble grapefruit flavonoid Naringenin: design, characterization, in vitro and in vivo evaluation

Abstract Naringenin (NRG), predominant flavanone in grapefruits, possesses anti-inflammatory, anti-carcinogenic, hepato-protective and anti-lipid peroxidation effects. Slow dissolution after oral ingestion due to its poor solubility in water, as well as low bioavailability following oral administration, restricts its therapeutic application. The study is an attempt to improve the solubility and bioavailability of NRG by employing self-nanoemulsifying drug delivery technique. Preliminary screening was carried out to select oil, surfactant and co-surfactant, based on solubilization and emulsification efficiency of the components. Pseudo ternary phase diagrams were constructed to identify the area of nanoemulsification. The developed self-nanoemulsifying drug delivery systems (SNEDDS) were evaluated in term of goluble size, globule size distribution, zeta potential, and surface morphology of nanoemulsions so obtained. The TEM analysis proves that nanoemulsion shows a droplet size less than 50 nm. Freeze thaw cycling and centrifugation studies were carried out to confirm the stability of the developed SNEDDS. In vitro drug release from SNEDDS was significantly higher (p < 0.005) than pure drug. Furthermore, area under the drug concentration time-curve (AUC0–24) of NRG from SNEDDS formulation revealed a significant increase (p < 0.005) in NRG absorption compared to NRG alone. The increase in drug release and bioavailability as compared to drug suspension from SNEDDS formulation may be attributed to the nanosized droplets and enhanced solubility of NRG in the SNEDDS.

Formulation development, optimization and evaluation of aloe vera gel for wound healing

Purpose: To formulate and optimize a herbal gel of Aloe vera extract containing Carbopol 934 as gelling agent and to investigate the effects of topical application of Carbopol 934 gel containing Aloe vera extract on the healing of skin wounds surgically induced in Wistar rats. Materials and Methods: Different concentrations of viscosity enhancer Carbopol 934 were tried and finally gel that showed good spreadability and consistency was selected for wound healing property of herbal gel of Aloe vera. Excision wound model was used for the study. Results: The optimized gel was evaluated for different physicochemical properties and wound healing property. Differences in wound healing were observed between the various treatments when compared to the control group. Tissue hyperplasia was lower in the control group compared to the other treated groups. In animals group treated with gel, 80.14% healing was observed up to 14th day. While in untreated group I (control) animals showed 52.68% healing of wounds on 14th day. On the other hand, control group animals also showed inflammation and pus formation up to 5th day of study, while treated animals did not showed any observable inflammation and pus formation. Conclusion: Results shows prepared gel has promising effect on the wound healing process.

Exploring scientifically proven herbal aphrodisiacs.

Procreation was an important moral and religious issue and aphrodisiacs were sought to ensure both male and female potency. Sexual dysfunction is an inability to achieve a normal sexual intercourse, including premature ejaculation, retrograded, retarded or inhibited ejaculation, erectile dysfunction, arousal difficulties (reduced libido), compulsive sexual behavior, orgasmic disorder, and failure of detumescence. The introduction of the first pharmacologically approved remedy for impotence, Viagra (sildenafil) in 1990s caused a wave of public attention, propelled in part by heavy advertising. The search for such substances dates back millennia. An aphrodisiac is an agent (food or drug) that arouses sexual desire. The hunt for natural supplement from medicinal plants is being intensified mainly because of its fewer side effects. In this review, we have mentioned the pharmacologically tested (either in man or animal or in both) aphrodisiac plants, which have claimed for its uses.

Enhanced dissolution and bioavailability of grapefruit flavonoid Naringenin by solid dispersion utilizing fourth generation carrier

Abstract Context: Naringenin (NRG), the aglycone flavonoid present in grapefruits, possesses anti-inflammatory, anti-carcinogenic, anti-lipid peroxidation and hepato-protective effects. However, it is poorly soluble in water and exhibits slow dissolution after oral ingestion, thus restricting its therapeutic efficacy. Objective: With the aim to enhance the dissolution rate and oral bioavailability of NRG, solid dispersion technique has been applied using Soluplus® as carrier. Methods: Solid dispersions of NRG were prepared by solvent evaporation and kneading methods using various ratios (1:4, 3:7, 2:3 and 1:1) of NRG:Carrier. Characterization of the optimized formulations was performed using Fourier transform infrared spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The in vivo behavior of the optimized formulations was also investigated in Wistar Albino rats. Results: NRG solid dispersion showed a significantly higher solubility and drug dissolution rate than pure NRG (p < 0.001) and it followed the Higuchi model. Among the different methods employed for the preparation of solid dispersions, solvent evaporation showed better drug release profile. DSC analysis indicated reduced crystallinity of NRG as no discrete peaks of NRG were observed. This was further substantiated by XRD analysis. Furthermore, area under the drug concentration time-curve (AUC) of NRG from solid dispersion revealed a significant increase in NRG absorption compared to NRG alone. Conclusion: Based on these results, it was concluded that solid dispersion technique markedly enhances the in vitro drug release and in vivo behavior of the grapefruit flavonoid NRG.

Anti HIV nanoemulsion formulation: optimization and in vitro-in vivo evaluation.

The objective of the present work is to develop a dose adjustable nanotechnology based liquid formulation of efavirenz with improved bioavailability for HIV therapy. Nanoemulsion of efavirenz was developed using phase inversion composition method with the help of ternary phase diagram. Globule size of the o/w nanoemulsion was studied with the help of dynamic light scattering and further confirmed with TEM analysis. Optimized formulations were subjected for in vitro dissolution studies and in vivo studies were done in rats to calculate pharmacokinetics parameters and compared with efavirenz suspension. TEM results revealed that the globule size of optimized formulation was less than 30 nm. In vitro release profile showed more than 80% release within 6 h which was highly significant (p>0.05) and pharmacokinetic studies also proved a promising in vivo absorption profile when compared to the efavirenz suspension. The developed nanoemulsion proved to be an effective dose adjustable formulation of efavirenz for pediatric HIV therapy.

Formulation of nanoemulsion: a comparison between phase inversion composition method and high-pressure homogenization method

Abstract There is lot of confusion in the literatures regarding the method of production of nanoemulsion. According to some authors, only the methods using high energy like high-pressure microfluidizer or high-frequency ultra-sonic devices can produce actual nanoemulsions. In contrast to this concept, one research group reported for the first time the preparation of nanoemulsion by a low-energy method. Later on many authors reported about the low-energy emulsification method. The purpose of this work is to formulate, evaluate and compare nanoemulsions prepared using high-energy as well as low-energy method. Nanoemulsions formulated were based on the phase inversion composition technique (low energy method) and were selected from the ternary phase diagram based on the criterion of their being a minimum concentration of Smix used in the formulation. For high-pressure homogenization method (high energy method) Design-Expert software was used, and the desirability function was probed to acquire an optimized formulation. No significant difference (p > 0.05) was observed in the globule size of formulations made by each method, but the value of poly-dispersibility index between the two methods was found to be extremely significant (p < 0.001). A very significant difference (p < 0.001) was observed in the drug release from formulations made by each method. More than 60% of the drug was released from all the formulations in the initial 2 h of the dissolution study.

Skin decontamination cream for radiological contaminants: Formulation development and evaluation.

Background: Increased use of the radioactive materials in the field of research, medical, nuclear power plant, and industry has increased the risk of accidental exposure. Intentional use of the radioisotopes by terrorist organizations could cause exposure/contamination of a number of the population. In view of the accidental contamination, there is a need to develop self-usable decontamination formulations that could be used immediately after contamination is suspected. Materials and Methods: Present work was planned to optimize and develop self-usable radiation decontamination cream formulation. Various pharmaceutical parameters were characterized. 99mTc-sodium pertechnetate was used as radiocontaminant. Static counts were recorded before and after decontamination using single photon emission computed tomography. Results: Decontamination efficacy of the cream was found to be 42% ± 3% at 0-0.5 h after the exposure. Primary skin irritancy test was satisfactory as no erythema or edema was observed visually after 2 weeks of the formulation application. Conclusion: The decontamination studies proved the potential of EDTA to remove the radiological contaminants effectively.

Chemical, biological, radiological, and nuclear threats-Decontamination technologies and recent patents: A review

With the increase in the intensity of threats perception and possibility of mass casualties in case of a chemical, biological, radiological, and nuclear (CBRN) emergency, there is a need to develop novel and effective systems for decontamination. The natural calamity in Japan leading to world’s most critical nuclear emergency exposed lack of decontamination formulation and technologies globally. There is a need to develop novel and effective systems for decontamination as the current technologies are expensive and cannot be used by victim themselves. Decontamination formulations that can be used by victims themselves are need of time. The review gives a brief introduction about the various CBRN agents and a concise discussion about the decontamination technologies available globally. The article also provides a review of the existing patents on the methods, equipment/devices used in CBRN decontamination.